Development of new Parameters for StructureDetermination and Dynamic Investigations on Biomacromolecules by NMR ...- ;.%,njv-zs j" -Z4 MASSACHUSETTS INSTITUTE, OF TECHNOLO", MAR 2 5 2005 by LIBRARIES Elke Duchardt Dipiphil mzt,Bidriste Unirsity fFrankfut Gernd 1999 SUBMITtED TO THE DEPARTMENT OF CHEMISTRY IN PARTIAL FULFILL OF THE REQUIREMENTS FOR THE DEGREE OF DOCIOR OF PHILOSOPHY IN BIOLOGICAL CHEMISTRY AT THE MASSACHIUSETTSINSTITUTE OF TECHNOLOGY Febary 2005 © 2005 Massachusetts Institute of Technology. All rights reserved. /'7 1. Author / x/ 1! V Department of Chemistry September 17, 2004 ,, Certified by Harald J. Schwalbe Professor of Chemistry Thesis Supervisor Accepted by Robert W. Field Department of Chemistry Chairman, Departmental Committee on Graduate Students This doctoral thesis has been examined by a committee of the Department of Chemistry as follows: •I Professor Robert G. Griffin r ) / k k, Chair Professor Harald J. Schwalbe Thesis Supervisor Professor JoAnne Stubbe ...-.. Development of new Parameters for Structure Determination and Dynamic Investigations on Biomacromolecules by NMR by Elke Duchardt Submitted to the Department of Chemistryin Partial Fulfillment of the Requirementsfor the Degree of Doctor of Philosophy ABSTRACT Nuclear magnetic resonance (NMR) spectroscopy is unique in the content of structural as well as dynamic information that it can provide at atomic resolution. The aim of this PhD-thesis was to contribute to the understanding of biochemical processes by means of NMR-spectroscopic techniques, targeting specific problems as well as contributing to the general understanding and providing new, widely applicable methods. The main focus was on the structural as well as dynamic study of ribonucleic acids (RNA). A new structural NMR method was developed aimed at the determination of the glycosidic torsion angle X in RNA, which defines the relative orientation of the nucleobases in respect to the ribose moiety (Duchardt et al., 2004). X was derived from the angle dependence of carbon-hydrogen dipole-dipole, nitrogen chemical shift anisotropy cross-correlated relaxation rates (F-rates). Method development comprised the design of a novel NMR experiment, the (HCN), as well as the parameterization curves. The novel method provides an accuracy of introduction of F versus around 10 degrees or better, comparable to the precision of conventional angle determination techniques. In contrast to conventional methods, the F(HC) is sensitive to molecular size and will therefore proof beneficial in the investigation of larger RNAs by NMR Apart from this methodological contribution to RNA structure determination, the dynamic properties of the abundant YNMG RNA tetraloop motif (with Y=C or U; N= any base; M=C or A) were studied in a residue specific manner by means of 3C NMR relaxation measurements. The dynamics of the extraordinarily stable cUUCGg motif were compared to the less stable uCACGg hairpin, which forms the stem-loop D (SLD) in the regulatory 5'-cloverleaf of coxsackievirus 3B. Measurements were carried out at 25°C, at which both motifs are stable, as well as at close to the melting point of SLD (43°(). Ribose and base moiety specific amplitudes and time-scales of motion were extracted from R1, R1 p and the heteronuclear nOe of Q6and CQ.in pyrimidines and CQand CQ.in purines by application of the model-free formalism (Lipari and Szabo, 1982). The application of the model-free formalism to C1., and C6 which possess an additional adjacent carbon spin, was examined for the uniformly isotope labeled RNA hairpins investigated in this study. In addition, the relaxation data analysis was optimized for the 13C chemical shift anisotropy based on chemical shift tensors available to date (Stueber and Grant, 2002;Fiala et al., 2000). While at room temperature, the dynamics closely follow the structural features of both hairpins, residues in the loop closing as well as in the adjacent basepair exhibit highly increased flexibility at temperatures close to the melting point of SLD. In contrast, loop dynamics remain unperturbed. In SLD, the residues close to the loop are conserved among the 5 family of rhino- and enteroviruses, indicating a sequence based mechanism of decoupling loop structure and stability in order to adjust to the twofold requirement of a defined structure for protein recognition and low stability to ensure efficient melting within the genomic transcription process. In addition to investigations on RNA, structural studies were also conducted on the C-chain of the T-cell receptor (TCR) in order to contribute to the elucidation of the early events in T-cell activation. According to earlier studies (Aivazian and Stem, 2000), the extracellular encounter of the T-cell receptor with an antigen is transmitted into the T-cell via a lipid induced structural transition of the TCR C-chaincytoplasmicdomain. In order to lend detailed structural support to the proposed mechanism, the structure of TCR 4 was studied in free solution and in the presence of detergent micelles. By means of standard NMR-techniques, the backbone assignment of both forms of 4 was achieved and secondary structural information was obtained. In addition, the binding site of the protein Nef of simian immunodeficiencyvirus (SIV) onto TCR ~ was determined. Thesis Supervisor. Harald Schwalbe Title:Professor of Chemistry References: Aivazian, D. and Stem, L. J. (2000) Nat Sta Bio, 7, 1023-6. Duchardt, E., Richter, G, Ohlenschlager,O., Gorlach,M, Wohnert, J. and Schwalbe,H. (2004)J Am(banSr, 126, 1962-70. Fiala, R., Czernek, J. and Sklenar, V. (2000) J Bind NMR, 16, 291-302. Lipari, G. and Szabo, A. (1982) JAm CaenSoc 104, 4546-4559. Stueber, D. and Grant, D. M. (2002) JAmCIemSc, 124, 10539-51. 6 "Themare a rmillionzs to get no signal" Harald Schwalbe "7n eejust muke nore scans" Christian Richter '"Still,Me iller gt as rch signl as ona Varian" Jens W6hnert 7 THANKS TO.... .... THE SUPERVISORS I am deeply indepted to my thesis supervisor, Prof. Harald Schwalbe. He taught me NMR, encouraged, supported my projects with his expertise, and especially in the last years of my thesis supported my increasing independence with occasional insightful discussions. Jens W6hnert, who would never allow me to call him anything close to my supervisor, has been of indispensable help to me ever since he joined the group. I would like to acknowledge his critical support concerning both specific as well as very fundamental aspects of my work his patience in telling me the same things over and over again (it did go both ways after all) as well as the readiness in supplying me with any type of literature. I also appreciate his cynical sense of humor. Thanks for reading my thesis so carefully and partly even twice. I would like to warmly thank Christian Richter for our inspiring collaboration and his continued support. It was due to his careful and friendly supervision during a lab-rotation that I decided to work in the field of NMR Later, collaborating with him in the field of pulse programming proofed very fruitful for both of us. In addition, his great memory for whatever he had ever done made my life so much easier, as did his easy manners and his continuous kindness, no matter if a shaped pulse was required or a ride home. .... THE THESIS COMMITTEE A am grateful to Prof. Bob Griffin, Prof. Barbara Imperiali and Prof. Joanne Stubbe for their support in the course of this thesis, in respect to science as well as in coordinating the whole procedure. .... THE JAN GUY I could not be more grateful for your cheerful temper during this last month of writing. Thanks for being there, making me worry less, getting me out for a coffee break, feeding me with junk-food and reading this stuff over and over again. You are the best. ....THE FAMILY I am deeply grateful to my mother, who always wanted me to go study and become a PhD. I am even more grateful that in the end she really believed, I would make it. Thank you for starting to study medicine, so you finally realized that I actually learnt something in the last ten years. My brother has been always there for me during all this time. He makes me ever so happy to have a sibling that I always walk around telling people they should have more than just one child. .... THE SISTERS IN ARMS Luckily for me, Joanna & Suman both started writing up when I did to share good sessions in the library, deep depressions about unproductiveness and nice coffee-breaks. Thanks guys, long live the Tripod! 8 ....THE OTHER PHD-STUDENT For five years, I sat next to Julia, first in Boston then in Frankfurt. That's why we had plenty of time discussing almost everything from science to an appropriate retirement plan. I cherish your honest opinions and the occasionalapple that I got from you. ....THE GIRLS-LAB I had a great time with Julia, Emily, Karla and Aph. Thanks for the special, girly atmosphere. Where else could I share my waist-line concerns and learn about tanning solutions? My special regards go to Aph, who became a friend and impressed me both by her dedication to her work and her great fashion sense. Thanks for your constant open ear for my worries. I also want to acknowledgeKarla, who is trying so hard to make sense of this thing called thesis at the moment. Don't worry, I did it, so you can, too. .... THE GROUP The continued good accord in the whole Schwalbe group rendered this PhD period a very pleasant time for me. The aptitude to help other group members, the sense of a common goal and the extension of the work group into private activities were really exceptional. Among all these people my special regards go to Christian Schlbrb, who was a very friendly and good humored fellow system administrator and will certainly do a great job in the future, if he doesn't decide to finish his PhD, Boris FiIrtig and Jonas Noeske, who were very good undergraduate researchers and fortunately decided to join the group and Elke Stirnal, who patiently purified my RNA on the HPLC Last but definitely not least, I would like to thank Frau Paulus, who is simply the best secretary ever and the gute Geist of the work group. The same goes for Zim, who was always there for helping out with the spectrometers or anything technical, which is amazing considering his difficult working environment. .... THE BOSTON PEOPLE My deep-feklt gratitude goes to my friends in Boston, who helped me to find a start in this new environment. You contributed a lot to the great experience that these two years abroad constituted for me, which I still remember in happy melancholy. Especially, I would like to thankJulie, the social wizard, who introduced me to squash as well as to her very diverse circle of friends and thus gave me an easy start. In addition, I want to acknowledge Peter and his great explorer spirit. If it wasn't for him, I would have never seen half as much of New England. He was also a great supporter during my time at MIT. I would also like to thank the people in the Magnet Lab for their enthusiasm and their friendliness, especially Ajay and Peter. I feel especially grateful to Chris Turner, who became a special supporter to me during my time in Boston and is one of the funniest people I have ever met. 9 TABLE OF CONTENTS Abstract ..................................................................................................................................... 5 Acknowledgement ................................................................................................................... 8 Table of Contents ..................................................................................................................... 10 List of Abbrev iations................................................................................................................ 13 CHAPTER 1: INTRODUC ON...........................................................................................15 The power of NMR 16 Basic principles .............................................................................................................. determination Structure Structure dtermination.................................................................................................1 17 19 Dynamic investigations .................................................................................................. 26 References-30 ...................................................................................................................... CHAPTER 2: F(HCN)-EXPERIMENT ............................................................................... 37 INTRODUC17ION 40 I........................................................................................................ The glycosidic torsion angle X 40 Determination of X by NMR 41 Determination of X from cross-correlation relaxation rates Parameterization of F(X) Definition of X in NMR structure determination Molecules under investigation: The 14-nt and the 30-nt RNA 42 44 45 45 MATERIAL AND METHODS.. 47 Sample preparation 47 NMR spectroscopy 47 F-rate calculation RNA structure calculation 49 49 51 ............................................................................................................ RE SULTS The quantitative F(HCN-experiment The quantitative F(H2'C2'N-experiment 51 68 1 CONCLUSIONS ........................................................................................................... 71 Pulse Sequence Development 72 Experimental Quality REFERENCES ............................................................................................. 75 10 CHAPTER 3: RNA TETRALOOP DYNAMICS .................................................................. 79 INTRODUCTION ,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,82 The tetraloop RNA secondarystructure motif Dynamic investigationson RNA by NMR 82 85 Autocorrelated relaxation rates Model-free formalism Motional models 88 89 92 MATERIALS AND MATERIALS ANDMETHODS...94 METHODS~~~..................................................................................9 NMR spectroscopy Relaxation data analysis RESULTS 94 96 99 ..................... Temperature dependence of the imino proton resonances 99 13C relaxation analysis 101 . DISCUSSION ........................................................ 131 Model-free analysis 131 Dynamics of the YNMG tetraloop motif 134 OUTOOK .139 ,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,140 REFERENCES CHAPTER 4: STRUCTURE OF THE TCR -CHAIN ........................................................ 145 INTRODUCTION.148 ~~........................................................................................................4 INTRODUCTION T-Cell Activation The TCR ;-chain TCR q /Nef interaction Protein backbone resonance assignment MATERIALS AND MATERIALS ANDMETHODS METHODS~~~..................................................................................15 148 149 150 152 154 Protein expression Backbone assignment of free TCR q Concentration dependent experiments Temperature dependent experiments ~/Nef interaction studies TCR q in LMPG micelles 154 154 155 155 155 156 RESULTS 5 ....................................................................... RESULTS ........................................ 157 TCR ~ in solution 157 TCR bound to IMPG-micelles 169 CONCLUSIONS ,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,,174 REFERENCES .,,,,,,,,,,,,,,,,,,,,,,,,,,176 11 APPENDIX ............................................................................................... 179 A1. CHAPTER 2: F(HCN)-Experiment ---- .............................................................. Pulseprograms F-rate calculation References A2. CHAPTER 3: RNA Tetraloop Dynamics. .............................................................. Pulse sequences Extraction of peak intensities 181 181 184 195 196 196 202 A3. CHAPTER 4: Structure of the TCR c-chain .......................................................... 203 Assignment of free TCR 4 at 278K Assignment of free TCR ~ at 317K Assignment of TCR tLMPGat 310K PUBLICATIONS 203 205 207 211 ............................................................................................................... 12 LIST OF ABBREVIATIONS 13C carbon- 13 15N nitrogen- 1H hydrogen- 1 (proton) 31p phosphorous-31 A adenine C cytosine CD circulardichroism cm centimeter CS chemical shift CSA chemical shift anisotropy CSI chemical shift index CV coxsackie virus DNA desoxyribonucleic acids F cross-correlated relaxation rate G Gauss G guanine hetnOe heteronuclear nuclear Overhauser enhancement HIV human immunodeficiencyvirus HSQC heteronuclear single quantum correlation spectrum Hz Hertz INEPT insensitivenucleus enhancement bypolarization transfer ITAM immunoreceptor tyrosine-basedactivation motif J scalar coupling constant K Kelvin KD dissoziation constant kDa kilodalton LMPG myristoyl-phosphatidyl choline MHC major histocompatibilitycomplex 15 13 MHz megahertz mM millimolar PM micromolar MQ multiple quantum MRI magnetic resonance imaging Nef negative factor nOe nuclear Overhauser enhancement ns nanoseconds NS number of scans ppm parts per million ps picoseconds R1 longitudinal relaxation rate R2 transversal relaxation rate RDC residual dipolar coupling RMSD root mean square deviation RNA ribonucleic acid S2 square of the generalized order parameter SIV simian immunodeficiency virus SLD stem-loop D TPPI Time Proportional Phase Incrementation SW spectral width Tc molecular rotational correlation time TCR T-cell receptor TMSP 3-trimethylsilyl propionic-2,2,3,3-d4 acid sodium salt TOCSY total correlation spectroscopy TROSY transverse relaxation optimized spectroscopy U uridine Amino acids are abbreviated using the common single letter code. 14 Chapter 1:Introduction CHAPTER 1 Introduction TABLE OF CONTENTS 1.1 The power of NMR ....................................................................................................................... 16 1.2 1.3 Basic principles ................................................................................................................................ Structure Determination............................................................................................................... 17 19 1.3.1 Structure determination process .......................................................................................... 19 1.3.2 Structural Parameters ............................................................................................................ 19 1.3.3 RNA structure determination .............................................................................................. 22 1.4 Dynamic Investigations ................................................................................................................. 26 1.4.1 The importance of dynamics in the structure-function relationship . ............................ 26 1.4.2 Dynamic information from NMR ...................................................................................... 28 1.5 References........................................................................................................................................ References301.5 References30 301.5 15 Chapter 1: Introduction 1.1 The power of NMR Nuclear magnetic resonance (NMR) spectroscopy constitutes a non-invasive technique that allows for the spatially resolved investigation of objects of the size of a view Angstrom up to the entire human body (Figure 1). Two fundamentally different techniques have emerged: While the observation of the same spin in different environments yields super-molecular spatial resolution in magnetic resonance imaging (MRI) and NMR niCat, the investigation of different spins in the In MRI, the spatial distribution as well same environment constitutes the basis of NMR sptrcpy. of water hydrogens is obtained within different tissues or cell as the specific properties compartments through the application of magnetic field gradients, thus creating highly resolved, non-invasive two- or three-dimensional images from opaque, water-containing objects such as the human body. MRI therefore constitutes a powerful medical tool both for research and for diagnostic purposes. NMR microscopy represents the high spectral resolution variant of NMR, allowing for the detailed study of objects of the size of a view millimeters down to individual cells. In contrast to other microscopy techniques, NMR microscopy does not require transparent objects and can be extended to the observation of specific compounds such as metabolites. --'.':-- ":' I. 'i::.' .i.... ..: . ... '.- -. ...'MRi.:: . ... '-..i'::.'.:' .:' "?'.: , .: '!'::.':;-::.' O ,- .'. . ,... ?....-......;.0,'-. -': ;: :'.''.:.. i-:1'~-":,? ~'-!' -.?/..: mm .i: ,.:, : <.::' . ~~~~~~~~~~... "':.-103' "i * ','. inm : spe ~SS4Oj~ > i . 1 ' 0** *-- ' V nm ; VN- :.' "''''" !;;, :; i- pmuo .... Figure 1:Sze rane of NMR tahm. 16 'N A i^. ! ..:: X- ': f'' s ,.NM;: ,,- Idt ,N:-- . ..... ..- '- '-<'f.:.".:''.:.:".:....' :~i 1.:.":~.".'. ':"- ~~~~~~~~~~~~~~... ' i.';'..'.:.. : .';.L. ..,:.;!;.:.;;! :'' ' ...;:",,i'v 'i... , .;',.D; : _ :- 2 -,,..'.: I; ' i;;.. Phttoy~ Chapter 1: Introduction The major disadvantage of MRI techniques lies in their relative insensitivity, which they share with all NMR-techniques. Hence, if substances other than the bulk water are to be observed, appropriate isotope labeling schemes have to be applied, while substances of low in ziw concentrations may not be detectable at all. In contrast to MRI techniques, which directly obtain an image of the investigated object from the spatial distribution of one kind of spins, NMR spectroscopy produces an indirect image of its object through the observation of different kinds of spins and their interactions. From a network of spinspin interactions, the image of the object is then reconstructed. The observation of different spins allows for the investigation of objects on the molecular level. Due to the lack of spatial resolution and sensitivity of this technique, homogenous sample conditions are required. Hence, while it is possible to conduct these studies under physiological conditions within the living cell [7], sample inhomogeneities within the cell render this method unfavorable. In addition, NMR spectroscopy is a rather insensitive technique and therefore requires high sample concentrations. Consequently, the lion's share of NMR spectroscopic investigations so far have been conducted in zto. To date, the use of isotope labeling techniques with 13C, 5 N [8] and 2H [9-11], the development of sensitivity and resolution enhanced NMR techniques [12-14], the provision of novel structural NMR parameters [15, 16] and the use of high field magnets have been combined to render the study of proteins of around 30kDa and oligonucleotidesof around 10kDa a routine task, while moleculesof up to 80kDa [17] can be studied in high detail in special cases. Due to their unfavorable relaxation behavior, membrane proteins are still difficult to study in solution state NMR spectroscopy. In contrast, solid state NMR allows for the study of membrane proteins within the physiologicalenvironment of lipid bilayers [18, 19]. This technique, however, still suffers from line broadening and low sensitivity compared to liquid state NMR. 1.2 Basic principles In the following, a brief introduction to the basic principles of NMR is given. For a general introduction to NMR, see ref. [20]. NMR experiments are based on the manipulation and detection of weak sample magnetizations that arises from the interaction of spin-carrying nuclei with a static magnetic field. The simplest NMR active nuclei are those with a spin of ½. Spin h nuclei can occupy either of two distinct energy levels or spin-states. In the presence of an external magnetic field, the degeneracy of these spin-states is removed. The spins will align either parallel (lower energy state) or antiparallel (higher energy state) 17 Chapter 1:Introduction to the magnetic field. In the classical picture, the spins can be imagined as precessing around an effector axis oriented along or opposite to the magnetic field. The precession frequency (Larmor- frequency) is the product of the magnetic field at the position of the spin and a proportionality constant y, the gyromagnetic ratio, which reflects the magnetic properties of the nucleus. Since the magnetic field experienced by a given nucleus constitutes the sum of the external magnetic field and the field generated by the surrounding electrons, resonance frequencies reflect the chemical composition as well as the conformational arrangement. Under equilibrium conditions, the higher population of the lower energy spin-state results in a weak excess magnetization oriented along the magnetic field, which can be manipulated by the application of radio-frequency pulses at a frequency close to the Larmor-frequency of the nuclei. By application of the appropriate pulses, the magnetization can be rotated into the plane transversal to the magnetic field, where its precession frequency can be detected. Due to their different Larmor-frequencies, spins in different chemical environments are detected at different frequencies, and spectra can be obtained. Since the Larmnor- frequency or resonance frequency of a spin is dependent on the spectrometer field-strength, the frequencies are normalized to the magnetic field and then called the chemical shift, which is quoted in parts per million (ppm). Perturbation of the equilibrium magnetization also constitutes the starting point for spin-spin interactions through different through-bond as well as through-space mechanisms (section 1.3.2). These effects give rise to spectral resolution in multidimensional spectra from the correlation of different chemical shifts. In addition, spin-spin correlations relate spins in space or through bonds and therefore constitute the basic principle of any structural NMR spectroscopic study. Spin 1h2 particles are the ones most widely studied by NMR. Apart from 1 H (protons) and 3 1p, the spin ½ isotopes of most elements occurring in macromoleculesare not very abundant. In the case of carbon and nitrogen, isotope enrichment techniques with 13C (natural abundance 1%) and "5N (natural abundance 0.4%) have been developed both for proteins [8] and nucleic acids [21-23]. 18 Chapter 1: Introduction 1.3 Structure Determination 1.3.1 Structure determination process Structure determination by NMR is based on the sequence of procedures depicted schematically in Figure 2. At first, a sample of the molecule of interest needs to be prepared in quantities of several milligrams featuring the desired isotope labeling scheme. In general, several samples with different labeling schemes are required. After preparation, the desired NMR spectra are obtained from the samples. Spectra analysis requires the resonance assignment in order to connect the resonances within the spectra to the spins in the molecule. The NMR parameters, on which the structural investigation is based, are then obtained from the assigned spectra and subjected to a structure calculation procedure. ......... . .I . -. mplo . -. -;r"paratlon. ,. .... '~.,'. : : :.:. .Spla-a $^ . Acquisition '-:;. ". "./. -* ~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~. Figure 2: Stmawued im . . Structure . Structure . . .. .:... -Calcultion 6616h~on byNMR. 1.3.2 Structural Parameters The acquisition of structural parameters from NMR-experiments is possible due to distance or angle dependent spin-spin interactions. The most common structural parameters are summarized in Figure 3 and briefly discussed in the following: In general, distance information is obtained exclusively from dipolar through space interactions (nuclear Overhauser effect or nOe [24). The intensity of a nOe between two nuclei is dependent on the inverse sixth power of the internuclear distance. Proton-proton nOes constitute the main source of information in NMR structure determination [25]. They, however, only report on distances smaller than 6 A and therefore fail to report on global structural arrangements. 19 Chapter 1:Introduction TRADITIONAL TECHNIQUES NEW TECHNIQUES I a I Figure 3: StructuralNMR paranreters and dxheir inpliatin instmcturedetemina The same applies to scalar coupling constants (J-couplings) [26]. J-couplings are angle dependent on through-bond interactions. While three-bond vicinal J-couplings (3J-couplings), which report on dihedral angles, represent the most widely used structural parameters [27], also geminal (2J)and onebond (J) couplings can contain a measure of structural information [28-30]. The structural content of scalar couplings cannot be extracted directly but relies on semi-empirical parameterizations, the so-called Karplus-equations [31]. For a number of structurally interesting J-couplings, e. g. for 3J(HNH-) in the protein backbone, these Karplus relations have been developed extensively[32-35]. Cross-correlated relaxation rates (F-rates) have only recently been introduced as structural NMR parameters [15] and since their introduction have found wide-spread application in structural studies on proteins and as well as nucleic acids [12, 36-41]. F-rates arise from the angle dependent through space interaction of two dipoles (Figure 3), a dipole and the chemical shift anisotropy (CSA) of a nucleus or two CSAs. Although the chemical shift anisotropy is averaged out in solution by rapid tumbling and only the isotropic chemical shift is observed, the CSA results in relaxation relevant fluctuating magnetic fields at the position of neighboring spin upon molecular reorientation. In principle, the information content of F-rates and 20 Chapter 1: Introduction J-couplings is redundant. Since F-rates are, however, through space in nature, they do not depend on through bond correlations and are in principal distance independent. Furthermore, while scalar coupling constants are independent of molecular size, F-rates are sensitive to the size and shape of the molecule as well as its dynamics. While these dependencies can complicate the structural interpretation of F-rates, in the study of larger systems their size dependence constitutes a major advantage compared to J-couplings. Residual dipolar couplings (RDCs) represent the most easily accessible and therefore most widely used long-range structural NMR parameter. RDCs report on the orientation of two dipoles in respect to a molecular orientation tensor (Figure 3) [16, 42, 43]. The dipolar interaction between two nuclei depends on the angle between the internuclear vector and the magnetic field and can be of the order of several Kilohertz. In isotropic solution, dipolar interactions are averaged out due to rapid molecular reorientation and are only maintained in the nOe and their contribution to nuclear relaxation. Weak alignment by orienting media such as phage or lipid bilayers leads to the adoption of a preferential orientation of a fraction of the molecules, thus rendering the measurement of scaled or 'residual' dipolar couplings possible. These RDCs are of the order of several Hertz and can be translated into structural information through a molecular alignment tensor, which defines the extent of alignment and the orientation of the molecule with respect to the magnetic field. Since RDCs describe the orientation of each dipole in respect to this alignment tensor, relative orientations between different dipoles can be obtained irrespective of the distance. Similar information to the ones obtained from RDCs can also be extracted in the same fashion from the CSA [44-46]. Apart from these spin-spin interactions, the chemical shift of a spin by itself is sensitive to its environment and therefore carries structural information. In proteins FL, Cu, Co and C chemical shift deviations from standard random coil chemical shifts measured semi-quantitatively in the form of the so-called chemical shift index (CSI) constitute a very sensitive probe for the presence of ahelical of 13-sheet secondary structural elements [47-49]. In addition, chemical shift changes constitute sensitive probes for structural rearrangements involved in conformational transitions or interactions. In this thesis, a structural investigation of the C-chain of the T-cell receptor has been carried out restricted to standard protein assignment experiments in order to obtain chemical shift based secondary structure information as well as to study the interaction site with the HIV-protein Nef (Chapter 4). 21 Chapter 1: Introduction 1.3.3 RNA structure determination Ribonucleic acids (RNAs) are composed of a sequence of four different nucleotides, adenosine (A), cytosine (C), guanosine (G) and uridine () (Figure 4A), linked by phosphodiester bonds. The ability of the nucleobases to form hydrogen bonded pairs constitutes the basis of secondary structure formation. While regions with Watson-Crick base pairs (A paired to U, C paired to G; Figure 4B) fold into helical duplex structures, loops are formed when the RNA strand folds back on itself and bulges arise from unpaired regions within the stem (Figure 4). These basic secondary structure elements are structured to a varying degree, involving non-canonical (non-Watson-Crick) basepairing as well as hydrogen bonding interactions of the ribose moiety and the phosphodiesterbackbone. ",~i' ~~ -.NH 2 A B - ... .. P' 0 , .:.: - .... . : .I.' .. '.' ''-.. , ':'.,: .. ..... ::":- ..,:' .. . .. . ,:.!):.i' " -. :i.:. Nucleo- N abase :(IA] : :' J N III i 0~ Phosphate IRibose IH Im.i.JI OH "H OH = i .--. r . ':... ... . .. NH 2 '". :::.-: --- ' . ... NI I I I . 1: , ; - I . I I . ., ,, ,. . ".:"": f-:" NH N' :'. ' u NH2 I . II I II Z. . : I Z . I . .I , . . . . II. I ., ,: : - --. i. ,: ...I I %5 1....%, I . ....Z ' . III C -.::--/..-~ ... ' .- "-:..-'--.... " Duplex , .. 0-- .0 ..... .. '- ..::..- :...-..":......:~.::!: ... Loop -- Base Base-pai .. :..:.. : '.- !.-'':': Bulge ''Three-way ' -I-I ; II Figure 4:RNA srumo A Nudetde sm .:.. ' .:..''.:..'.. '=.- ;'' ~.:"i' :'."'..l', Four-way IJunction Junction | = .-- .:.-:';..".:.. ' G-Quartett ', Guanine. i 2'I~~~~~~~~~~~~~~~~~7 J~l 00S_10 J=QI0l 7? B: WatscnCride basepas. C Semdarystru senivysctim nag (nit). andnve owplwaiud 22 h boxks (left) Chapter 1: Introduction Apart from a small number of special secondary structure motifs, like the G-quartett, more complicated secondary structure arrangements such as three- or four-way-junctions (Figure 4C) can be derived from these three basic secondary structure motifs. Since the investigation of RNA by multidimensional heteronuclear NMR methods was made 3C possible due to the development of techniques for the preparation of and "5 N isotope labeled RNA in 1992 [21-23, 50], a large number of NMR experiments has been devised [51, 52] aimed at improving the accuracy of NMR-derived RNA structures. However, the size-limit of RNAs studied routinely by NMR is still restricted to around 10kDa (- 30nt). This size limitation is due to the inherent low spectral resolution of oligonucleotides. As depicted in Figure 5A for a 10-nt RNA with 3C selective labeling of the four loop residues [53, 54], the poor spectral resolution of proton 1D spectra can be overcome by 2-dimensional correlations with the attached carbon nuclei. A B ]IFtnhII IJ 11 '-U | .. U.' . ;,..- Cl, U u Cc .-.' -.U . . .' - .. .. C-G .. ,- G!' . . . '- ..-'' i' .;:.'HS";:'.: u^Jf .-..ui. !. .... ... .:.:i.i . .-'.:---U -' ., .;.'-.. .. . : N..... .;. ~~~~~~~ .";".-i: .. / ~~~~~~~ ... . .... . ° - * : 1..C.... t- ....... 6.0 .5 - - : . 5 : G ' .' .45 -.';.:..'., .... ... C . .. .: .. . ;-..:. ......... -sc .... .. . ~~~~~~~~~65- : .... 1H-- - 4 s , .....,.,,..,.. ~C5'/H5',H5" --- : .. a. . '.... ... :.... .... -.. .... ... C2'/H2' C3'/H3'... -'=75.... ..7 .: ' . '.~ '.,':';,-1: .-C '.: :G ' '-:.: :1,'J .'.'501.':.. G-G 6a :-.' '.'. 55 -. : :. C4!IH4' ::-C'/H1'..: ' " ....... -:.... .. ... . . ... .:.0 5 .:5,0'4.4 ~~~~~~~~~~ Figure 5: 1Dprnm spenn ad (t) 13Claktbeling in thef ..... ':'--3:'.'.: ". -'.'!.:".: ".. ".. .... :. -AC -G UA ::-G-C - ; ;:-.. 4.5- U" :' . ..... . ..... " .:....; '.... .s. ... ... . . - 4:-.-': :. 4,5 ....... :.^.,^.,..... .--,.u;* 'H, 5~~~~~ - :. .. C:"... ............ .A 85:'; ,' -1-4. ,-! .-. :92 .'. " -: 4 1CI 5' (t qfd' e risberamties f a 10-nthapn lct residues (). 'H, 13C-ordati (H, C- rgi of afidly '13Clali RNA haitpin The lo ard dosingbasepairresiduesarehigblild in de speanan 23 .. ..'..::..' 3' ithsdect 14-nt (B) ard 30-nt (C) Chapter1: Introduction In contrast, for larger molecules, like a fully 13Glabeled 14-nt (Figure 5B) and a 30-nt hairpin RNA (Figure 5QC,the spectral resolution becomes increasingly poor. Dispersion is obtained mainly for the non-canonical loop regions, which exhibit structure specific resonance patterns (see grey shaded resonances in Figure 5B,C), while the resolution of canonical duplex structures resonances is small. Spectral overlap arises from the small number of building blocks of partly similar or even identical chemical constitution as well as the limited diversity in secondary structural motifs. Although spectral crowding can be overcome by the application of elaborate selective isotope labeling schemes [53], this is work as well as cost intensive. A B 1 ... .: .. ,. , .. '. :' "'., ., . C . .. l I . ... , : ,: o Figure 6: Tosionangl (4) andNMR-atew mndez (B) in dtephapt ter dei ck and e riboie ty ofRNA. C Basesin RNA. The mdedzsf arepai it tir pesiz WatsmoCrideKdren b g panrs; amiei (A) it uradle (U) and guarni (G) amaddioUy mk edby ba ithcyeid (C). Pnta are shded in gre prom, ubich armecang str . 24 uith thesdolet O er Chapter 1: Introduction In addition to the problem of spectral resolution, the density of structural NMR parameters in RNA is small compared to its degrees of freedom In the absence of conformational averaging, the structure of a single oligonucleotide can be described by six dihedral angles (-c) in the backbone, two parameters for the cyclic ribose (the pseudorotation phase P and the maximum amplitude v-) and the glycosidictorsion angle X, which defines the orientation of the nucleobase in respect to the ribose (Figure 6A). Due to the depletion in NMR-active nuclei (Figure 6B), the backbone conformation cannot be sufficiently described by conventional NMR parameters such as 'H-H nOes and lHI,1H-, 13G and 1H,3 1P-coupling constants. In particular, the angles a and ( cannot be determined. Only recently, a method based on GH dipole-dipole, 31 P-CSA cross-correlated relaxation has been developed to address a and 4 [55]. In contrast, the ribose conformation can be determined from homonuclear 3J(H,) coupling constants [56-58] or GH dipole-dipole, C-H dipole-dipole cross-correlated relaxation rates [59, 60]. In the case of conformational averaging, heteronuclear 3 J(CH) and 2J(C,) coupling constants [2, 58, 61, 62] can complement the structural characterization of the ribose. The glycosidic torsion angle X, is conventionally determined from nOe intensities between base and ribose protons [63] or 3J(C,) coupling constants [64-66]. The advantages of a new method based on GH dipole-dipole, N CSA cross-correlated relaxation rates [1] developed in the course of this thesis, are discussed in Chapter 2. Within the planar nucleobases, the number of protons is also scarce (Figure 6). In addition, the solvent exchangeable amino and iino protons cannot be detected unless stabilized by hydrogen bonding. The participation of a base imino proton in a hydrogen bond is hence demonstrated by the appearance of its resonance in the NMR-spectrumr In addition, the hydrogen bonding partner can be characterized by exploitation of the partial throughbond nature of hydrogen bonds, which gives rise to a scalar coupling between the donor and the acceptor nucleus [67]. As described in detail above, further interresidual structural parameters can be obtained from homonuclear nOes and RDCs. 25 Chapter 1: Introduction 1.4 Dynamic Investigations 1.4.1 The importance of dynamics in the structure-function relationship In the enterprise of understanding physiological processes, it is in general easier to find out bat something is doing than to elucidate how it exerts its function. In order to understand molecular function, detailed structural knowledge is indispensable. It is, however, a common feature of all structure elucidation techniques like NMR, X-ray or electron microscopy that they report only on either the averaged structure or the most populated structure, depending on the time-scale of However, due to their intrinsic flexibility, molecules do not exist in one interconversion. conformation alone but in an ensemble of structures, which is characterized by the populations of the respective members as well as the rates of interconversion. While in some cases the limited information obtained from an averaged structure proofs sufficient to understand a mechanism (Figure 7A), in others the average structure fails to explain the function (Figure 7B). Averaged Structure Function Structural Ensemble ....... . ..... - .-. -. .. Averaged Structure Structural Ensemble Function ............... '' -,':,'',',!''': .... - ,-, . -: - a'-- -, " : B ~~~~b. f : ..- <:: /: -_ :- ,, . . '.. ....... - ' : 1. .:.:, . , :.: ' , .- : ', '., ' '.' .: ..--. : .:-- ' . §. 'a', ' < ' .. ,,, .': - '' ' , . . '' '" / , -Ai ; '' ., . -: -' .,. '- .'^' ''. . 7, .; -, :, : , '. , .'- :.,: ......... . :. 1, .,,: '1: ' .:" . ': : .; . ' '. .. ,: ss ............................ ,' _JJj,,_','. ' d',' -,'M§,-',x'''. ! ;;; . A- - hi:, * ., ., a.,,.,,-.,2.-, ., ,...:, . s . .. -': * .'. ............. - : ' . ' ,' ': . i, . I'd:'. 44A -''; ,: ''''.'' ".,''''''k'' ^ '., : A-. . :-,'-! ' ' .':' : j .. f....: . . .. - ' . ... ,,: . .-' ''-.'-''-... ., '-.1' , - .' . ' -- 9'; -- -;'' ', ' '';: ', ', -. ', ,: '^ .:"..' ,'. :. Figur 7 S tw-Fai .)...:,:.-.. :.- :: ':. S , - --- : .- .. ^' ., .: . :',, -.'.:. Thou',:... ... . - - -. :, - -- :. , rdatiomhp (4 andStuaural EmenbleF wtkn ndatimhp (B). 26 Chapter 1: Introduction A very prominent example for the break-down of the simplifying structure-function relationship can be found in the catalysis mechanism of peptide bond formation in the ribosome. Despite the availability of high resolution crystal structures [68, 69], the exact mechanism of catalysis is still highly under debate [68-73]. Also for a number of enzymatically active RNA molecules (the hammerhead ribozyme [74-76] and the lead dependent enzyme [77, 78), the averaged structure alone was insufficient to understand the proposed catalyticmechanisms. In these cases, the active form of the molecule, in which it exerts its function, constitutes a state within the structural ensemble, which is not observed in the structural investigation. In order to detect this active conformation, the equilibrium within an ensemble can be perturbed in a way that the active species become directly observable (Figure 8). An example for this strategy is the trapping of enzyme transition states by binding to substrate analogs mimicking the transition state. Apart from that, a possibility of assessing the entire conformational space accessible to a molecule is to study its dynamics (Figure 8). Dynamic investigations can be carried out without perturbation of the system and provide indirect information about the structural ensemble through amplitudes and frequencies of deviations from the averaged or most populated structure. Therefore, dynamic information constitutes the key for deconvoluting of the structural average into an ensemble of states (Figure 7B). Dynamics Trapping :'''-.' 1. '' -- ;-,. ' ......... i. -.- '. ,: - - . - --/ ................. --!5;.."-; --.'-- i i .' : A f-.Ad d . ; ,, , . , . . - S . . . . .- J Figure 8:Medxs fr st om f emenii.er. For proteins, the importance of non-equilibrium conformations for exertion of function has been derived from the correlation of enzymatic activity and conformational flexibility in enzymes from thermophilic and mesophilic organisms [79, 80]. While these homologues exhibit widely different temperature optima, internal dynamics are similar at maximum activity. The requirement of a certain measure of flexibility for enzyme activity was assessed from the dynamic information obtained by 27 Chapter1: Introduction various techniques such as neutron scattering [81-83], NMR hydrogen-deuterium exchange [80, 81, 84-90], NMR relaxation measurements [79, 91] and molecular dynamics simulations [92-95]. For RNA, the binding mode of TAR RNA to the Tat protein in HIV could be identified as a conformational capture rather than an induced-fitmechanism by demonstratingthat the bound form of the RNA already constitutes a part of conformational ensemble of the free molecule [96]. In this case, the structural ensemble was studied by the dynamic information included in residual dipolar couplings. This finding indicates that ground state flexibility might constitute the key precursor of adaptive binding, which is ubiquitously observed for RNA-protein interactions, and demonstrates the importance of dynamic investigations for the understanding of fundamental biochemical processes. 1.4.2 Dynamic information from NMR NMR-spectroscopy is sensitive to motions within a wide range of time-scales (Figure 9). In principle, every structural parameter also contains dynamic information due to its inherent sensitivity to structural changes. Apart from these side-effects of mainly structural parameters, a number of purely dynamic techniques have been developed. ,r I ... Z" I- 1012 10-9 1o-, 10-3 10 ° 103 Ai;i Figure 9: Timsades qfndear nar 28 andNMR-MJ e. Chapter 1: Introduction Different techniques exhibit sensitivity to different motional time-regimrnes.Thus, hydrogendeuterium exchange rates report on the dynamics of solvent-exchangeable protons such as amideand imino-protons on the time-scale of seconds to days. Autocorrelated spin relaxation rates (R1, R2 and the hetnOe) are sensitive to motions in the picosecond up to nanosecond range. In addition, R2 rates as well as ZZ-exchange spectroscopy contain information on slower dynamics in the millisecond regime. Furthermore, scalar couplings, cross-correlated relaxation rates, the nOe and residual dipolar couplings are all sensitive to motions in the millisecond regime. Due to their sensitivity to a wide range of time-scales, autocorrelated relaxation rates constitute a valuable tool for dynamic investigations,especiallyfor the study of fast internal motions. In contrast to dipolar couplings, they can be measured without perturbation of the sample with aligning media. In this thesis, autocorrelated relaxation parameters have been obtained for an abundant RNA secondary structure motif and translated into time-scales and amplitudes of motion in order to gain insight into the motifs function. 29 Chapter 1: Introduction 1.5 References 1. Duchardt, E.; Richter, C; Ohlenschlager, O.; Gorlach, M.; Wohnert, J.; Schwalbe, H. (2004). Determination of the glycosidicbond angle chi in RNA from cross-correlated relaxation of CH dipolar coupling and N chemical shift anisotropy. JAm ChemSoc, 126, 1962-1970. 2. Duchardt, E.; Richter, C; Reif, B.; Glaser, S. J.; Engels, J. W.; Griesinger, C; Schwalbe, H. (2001). 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CQl, 81, 991-1002. 76. Scott, W. G.; Murray, J. B.; Arnold, J. R.; Stoddard, B. L.; Klug, A. (1996). Capturing the structure of a catalytic RNA intermediate: the hammerhead ribozyme. Sdeaze,274, 2065-2069. 77. Hoogstraten, C G.; Legault, P.; Pardi, A. (1998). NMR solution structure of the lead- dependent ribozyme:evidencefor dynamicsin RNA catalysis.JMd Bid, 284, 337-350. 34 Chapter 1: Introduction 78. Wedekind, J. E. and McKay, D. B. (1999). Crystal structure of a lead-dependent ribozyme revealing metal binding sites relevant to catalysis. Nat Stna Bid, 6, 261-268. 79. Butterwick, J. A.; Patrick Loria, J.; Astrof, N. S.; Kroenke, C. D.; Cole, R.; Rance, M.; Palmer, A. G., 3rd (2004). Multiple time scale backbone dynamics of homologous thermophilic and mesophilic ribonucleaseHI enzymes.J Md Bid, 339, 855-871. 80. Zavodszky, P.; Kardos, J.; Svingor, Petsko, G. A. (1998). Adjustment of conformational flexibility is a key event in the thermal adaptation of proteins. Pnx Nad A cad SaciU S A, 95, 7406-7411. 81. Fitter, J. and Heberle, J. (2000). Structural equilibrium fluctuations in mesophilic and thermophilic alpha-amylase. Biqh)s J, 79, 1629-1636. 82. Fitter, J.; Herrmann, R.; Dencher, N. A.; Blume, A.; Hauss, T. (2001). Activity and stability of a thermostable alpha-amylase compared to its mesophilic homologue: mechanisms of thermal adaptation. Bixnistry, 40, 10723-10731. 83. Tsai, A. M.; Udovic, T. J.; Neumann, D. A. (2001). The inverse relationship between protein dynamics and thermal stability. Bis J, 81,2339-2343. 84. Kanaya, S. and Itaya, M. (1992). Expression, purification, and characterization of a recombinant ribonuclease H from Thermus thermophilus HB8. J Bild Cem 267, 1018410192. 85. Wuthrich, K.; Wagner, G.; Richarz, R.; Braun, W. (1980). Correlations between internal mobilityand stabilityof globular proteins. Biq)s J, 32, 549-560. 86. Wagner, G. and Wuthrich, K. (1979). Correlation between the amide proton exchange rates and the denaturation temperatures in globular proteins related to the basic pancreatic trypsin inhibitor.JMdo Bid, 130,31-37. 87. Delepierre, M.; Dobson, C M.; Selvarajah, S.; Wedin, R. E.; Poulsen, F. M. (1983). Correlation of hydrogen exchange behaviour and thermal stability of lysozyme. J Md Bid, 168, 687-692. 88. Varley, P. G. and Pain, R. H (1991). Relation between stability, dynamics and enzyme activity in 3-phosphoglycerate kinases from yeast and Thermus thermophilus. J Mo Bid, 220, 531538. 89. Hollien, J. and Marqusee, S. (1999). Structural distribution of stability in a thermophilic enzyme. PrxNad A cadSi US A, 96, 13674-13678. 90. Svingor, A.; Kardos, J.; Hajdu, I.; Nemeth, A.; Zavodszky, P. (2001). A better enzyme to cope with cold. Comparative flexibility studies on psychrotrophic, mesophilic, and thermophilic IPMDHs. JBid Gnx 276, 28121-28125. 91. Hernandez, G.; Jenney, F. E., Jr.; Adams, M. W.; LeMaster, D. M. (2000). Millisecond time scale conformational flexibility in a hyperthermophile protein at ambient temperature. Prc NadAcadSd USA, 97, 3166-3170. 92. 93. Lazaridis, T.; Lee, I.; Karplus, M. (1997). Dynamics and unfolding hyperthermophilic and a mesophilic rubredoxin. Prwin S/, 6, 2589-2605. pathways of a Tang, K. E. and Dill, K. A (1998). Native protein fluctuations: the conformational-motion temperature and the inverse correlation of protein flexibilitywith protein stability.J Biond StnaDyn, 16, 397-411. 35 Chapter1: Introduction 94. Colombo, G. and Merz, K. M. (1999). Stability and activity of mesophilic subtilisin E and its thermophilic homologue: insights from molecular dynamics simulations. JAm Gem Soc, 121, 6895-6903. 95. Grottesi, A.; Ceruso, M. A.; Colosimo, A.; Di Nola, A. (2002). Molecular dynamics study of a hyperthermophilic and a mesophilic rubredoxin. Prinm, 46, 287-294. 96. Al-Hashimi, H. M; Gosser, Y.; Gorin, A.; Hu, W.; Majumdar, A.; Patel, D. J. (2002). Concerted motions in HIV-1 TAR RNA may allow access to bound state conformations: RNA dynamics from NMR residualdipolar couplings.J Md Bid, 315, 95-102. 36 He .. Chapter2: F(HCN)-Experiment CHAPTER 2 Determination of the glycosidic torsion angle X in oligonucleotidesfrom GH dipole-dipole,N CSA cross-correlated relaxation rates 37 Chapter2: F(HCN)-Experiment Specific aims The aim of this part of my research was to introduce a new method for the determination of the glycosidic torsion angle %in oligonucleotides based on GH dipole-dipole, N CSA cross-correlated relaxation rates ric ' c s A D (cNs ). Three slightly different methods were investigated, all relying on .For the first time, F-rates were introduced as a ayt use structural parameter. A number of simplifying assumptions were applied and investigated in respect to their effect on the accuracy of the technique. In order to evaluate the new methods, they have been applied to two RNA molecules of similar secondary structure but different size (14-nt and 30-nt). Investigation of the same structural motif within two molecules of different size rendered it possible to assess (i) the quality of the underlying parameterization and the validity of the simplifying assumptions, and the sensitivity and possible molecular size limitations of the method (i) ,both in comparison to each other and to the currently available torsion angle determination method from 3 J-couplingconstants. In order to test the relevance of the new parameter, it has been incorporated into a structure calculation process. TABLE OF CONTENTS 2.1 INTRODUCTION .................................................................................................. 40 40 2.1.1 The glycosidic torsion angle X............................................................................................ 2.1.2 2.1.3 41 Determination of X byNMR .............................................................................................. 42 . ......................................... Determination of X from cross-correlation relaxation rates 2.1.3.1 Determination of Xfrom rFC' cs 1 1 9 . ................................................................ 42 .43 rCocs4 . . ............. DcsA9 and "C6/868,N1/9.43 2.1.3.2 Determination of Xfrom the ratio of r C1'HI',Nl9 A ........................................................................ 43 2.1.3.3 Determination of X;from r' o ~CD 2.1.3.3 Determinationof Xfrom pDDTCSA 4 ... 44 ................................................................................................... 2.1.4 Parameterizationof r(X). . 2.1.5 Definition of X in NMR structure determination 38 ....................................... 45 Chapter 2: F(HC-Experiment 2.1.6 2.2 Molecules under investigation: The 14-nt and the 30-nt RNA . .................................... 45 METHODS AND MATERIAL ............................................................................... 47 2.2.1 2.2.2 Sample preparation ............................................................................................................... 47 N MR spectroscopy .............................................................................................................. 47 2.2.2.1 F(HCN)-experiment ........................................................................................................ 47 3J(C,H) 2.2.2.2 coupling constants .............................................................................................. 48 2.2.2.3 Autocorrelated relaxation rates ...................................................................................... 48 2.2.3 F-rate calculation .................................................................................................................. 49 2.2.4 RNA structure calculation ................................................................................................... 49 2.3 RESULTS ................................................................................................................. 51 2.3.1 The quantitative F(HC -experiment ............................................................................... 51 2.3.1.1 Pulse sequence .................................................................................................................. 51 2.3.1.2 Derivation of F(X) parameterizations ........................................................................... 55 2.3.1.3 Determination of Xfrom rFHD,CSj ........................................................................... 59 2.3.1.4 2.3.1.5 2.3.1.6 2.3.1.7 Determination of X from F-ratio.................................................................................... 61 15 The N CS-tensor in solution from F-base..................................................................63 Transfer to larger systems ............................................................................................... 65 Incorporation of rF,,CSA into RNA structure calculation .................................66 2.3.2 The quantitative F(H2'C2N-experiment ........................................................................ 68 2.3.2.1 Pulse sequence .................................................................................................................. 68 2.3.2.2 Resolving X angle ambiguities with r 2DDCAI 9 .........................................................69 2.4 2.4.1 2.4.2 2.5 CONCLUSIONS ...................................................................................................... 71 Pulse Sequence Developm ent ............................................................................................. 71 Experim ental Quality ........................................................................................................... 72 REFERENCES ........................................................................................................ 39 75 Chapter 2: F(HCN)-Experiment 2.1 INTRODUCTION 2.1.1 The glycosidic torsion angle X Purines Pyrimidines X 27 Figwr 1:D az ofantiandf5 ,fm pyinid (nit) lia inRNA amgwnfordz 7hepiaur hIs kbenmr4 1 raw f X (nid). Stel lyprd o5mun i di pptu wanw rihe mg forpum (I) and leaidz,C2-andCye rla fumEr/[1l]. The torsion angle X in oligonucleotides is defined as the dihedral angle between C4 , N9 , C1 . and 04 in purines and C2 , N1 , C1, and 04 in pyrimiidines. It describes the orientation of the nucleobase with respect to the ribose moiety. The nomenclature for X is given in Figure 1 [ 1]. The sterically possible X angles in nucleotides are base-type and ribose pucker specific (Figure 1). Figure 2 shows the angle distribution for the different nucleotides within the large ribosomal subunit [2]. I jnos ziJI I -1 7n/) _/I.I!i, I I 0 90 ! 180 r 270 270 360 360 x [oN Figure2: argledisbution in thelaresuboutoftheriha e[2]. 40 Chapter 2: F(HCN)-Experiment In general, the angle distribution is more disperse for purines than for pyrimidines.Not only is the distribution broader in the ant region, which is the conformation in canonical stem regions, but purines are also more often found in the non-canonical syn conformation. 2.1.2 Determination of Xby NMR By NMR, the glycosidictorsion angle can be determined from the distance information contained in the intensity of the H 1-H 6 (pyrimidines) or H1 -H 8 (purines) cross peaks (Figure 3) in a NOESY spectrum with an accuracy of about + 50 ° [3], resulting in a qualitative discrimination between the syn and the ami conformation. NH9 N nOe J(C,H) OH Figure 3: CGulid ndn fiane of adne Forpyriidir, OH fr * anle detemntin by NMR. he irteraig nudeiare inat z dn e nt maei in ehse are H6forhe xnoe andC6ad C4 for in the kdar e3(C,H) wplirg Ct7stM5. A more accurate determination of X can be achieved from a more detailed nOe analysis including the H2-H61 8 and H3-H6 /8 nOes [3]. However, this analysis is very time consuming and not very precise due to various effects such as spin diffusion. Alternatively, can be derived from the interpretation of 3 J(C2/4 ,H) and 3J(C6 / 8,H1 ,) coupling constants (Figure 3) [4-6]. Recently, refined Karplus equations have been provided for 3 J(C,H 1 ), 3 J(C ,H ), 3 J(q,H.) 4 1 and 3 J(C,Hl) for the different nucleotides of DNA [6]. However, the validity of these equations for RNA still remains to be investigated. In addition, coupling constant determination is prone to systematic errors for larger molecules [4, 5]. 41 Chapter2: F(HCN)-Experiment 2.1.3 Detenrmination of Xfrom cross-correlation relaxation rates 2.1.3.1 Detenrmination of from Cl,1CS,9 The cross-correlated relaxation rate (F-rate) between the q,.-H 1 . dipole-dipole vector and the chemical shift anisotropy (CSA) of N1 in pyrimidines or N9 in purines, FCDm I , 9 (Figre 4A), is sensitive to the glycosidic torsion angle. (TN 33 OH OH CY1 A Figum 4: Sdxzi nomr N2 U22C '-22 B cF rentati DDcsA (4) and , DDCSA OH OH a I (inaden C B. orad an nawe~id~CHI',NI/9 In the simple case of isotropic molecular motion and isotropic fast time-scale internal motion, GH dipole-dipole, N CSA cross-correlated relaxation rates are given by Eq. (1) [7]: rF D,CSA = _ P (1) HN 154; o rNYr Y hS 2 T, r(Ho, *[cl (3cos2 c -1 ) + 42 (3cs 2 02 e -1)+ 33(3cos 33 )] In this, u is the permeability of the vacuum; h is Planck's number divided by 27; O(Nis the nitrogen Larmor frequency, yi is the magnetogyric ratio of the nucleus i; rH is the length of the CH dipoledipole vector, is the rotational correlation time of the molecule; S2 is the generalized order parameter, cri is the ith component of the fully anisotropic nitrogen chemical shift tensor (CS- tensor) and 0ic H ' N are the projection angles between the C-H dipole-dipole vector and the it 42 Chapter 2: F(HCN)-Experiment ' are component of the nitrogen CS-tensor. In the case of cm r nteCIH1',NI9 DD,csa the projection angles OiCHN dependent on X (Figure 4B). Eq. (1) shows that the angular interpretation of rF7' 9 depends s on the knowledge of the 15N CS-tensor of N1 and N9 in general as well as the individual motional properties of the molecule represented by S2 and -. In order to acquire S2 and c, separate autocorrelated relaxation rate measurements have to be carried out for each molecule under investigation. 2.1.3.2 Determination of Xfrom the ratio of rCCI'',N1/9 DDCSA and rcDCsA 8H6/8,N/9 Determination of addition to FCoIN/ becomes independent of 9 . c, if rC6D1'N19 (Figure 4 C8H6/,19Fiue4)iacurdn is acquired in In contrast to the latter, the F-rate between the C-H dipole-dipole vector in the nucleobase adjacent to the glycosidiclinkage (C6H6 or CgH) and the CSA of the nitrogen in the glycosidic linkage (N1 or N) D,~CSA I/ 9 ' rC,'HIN 19 andDS and 'c68H68, 6 NI/9 reports on a conformationally rigid unit. The ratio between (F-rtatio)is givenby Eq. (2): S2 DDcsA (2) rCHP.N C 'HI'.N f, DD,CSA C6/H6/ 8 ,N 2 C6/8H6/8N * Cr (3cos 20 C'H',N -1) + a (3COS2Ci'H (3cos1)+UN 20CrH',N _I) Orl {DO 11 '-l)+'22 "22 033 33$ o (3cos 2 C H6/8,N - 1)+ N (3cos 2 9 C6/8H6/8,N _1)+ aN (3cos 2 C6/8H6/8,N _1) Vl I1 22 "22 ' 33 v33 Under the assumption that the relative motion of the CH dipoles in the ribose and the base moiety can be neglected and therefore S1HN ScrmH,,Nandan C6/8H6/8,Nar are similar, the F-ratio is only dependent on X and the characteristicsof the nitrogen CS-tensors. 2.1.3.3 Determination of from rC' o CSA 9 "C2'Hl',N19 As for 3J coupling constants the angle dependence of F is degenerate. In order to remove this degeneracy, additional CD' 2tcD2vH, N/ 9 dependent parameters have to be obtained. The determination of Figure 5) (Figure 5) provides provides an an additional additional X sensitive sensitive parameter parameter and and is is methodologicaysimar methodologically similar to to 43 Chapter2: F(HCN)-Experiment the measurement of rF ' 1, 1 9 However, due to the additional dependence of this F-rate on the ribose pucker mode, it can only be applied in cases where the ribose conformation is characterized and rigid. NH, rtae otf Figure5:S·eic 2, NI/9 2.1.4 Parameterization of F(X) In order to translate the measured F-rates into values, F(X) parameterizations need to be established. The level of detail involved in the interpretation of F-rates depends on the extent of structural and dynamic molecular information included in the analysis. In contrast to coupling constants, F-rates depend on the apparent size of the investigated moiety, signifyingthat they are dependent on the size and the shape of the molecule as well as its internal dynamics. Furthermore, " DDCSA HCN -rates depend on information about the purines. For oligonucleotides in solution, no N -tensors of N in pyrimindines and N in 1 5N CS-tensors have been determined so far, since the chemical shift is averaged due to rapid tumbling and the measurement of a fully anisotropic tensor therefore requires elaborate experimental schemes. However, nitrogen CS-tensor values and orientations reported for mononucleoside crystals determined by solid state NMR [8] can be used in the parameterizationof rFCSA . In order to introduce F-rates as n touse structural parameters in the same way as coupling constants, it was assumed that (i) 15N CS-tensors obtained for mononucleosides in the solid state can be applied to oligonucleotides in solution and effects stemming from (ii) anisotropic diffusion, () internal motion (S2 =1), and, in the case of the F-ratio, (iv) differential motion between the base and the ribose moiety can be neglected. 44 Chapter2: F(HCN)-Experiment 2.1.5 Definition of X in NMR structure determination In conventional RNA structure determination by NMR the glycosidic bond angle X is restricted to either syn or anti from the analysis of the HI-H6/ 8 nOe. X angle restraints determined from the measurement of F-rates offer a way to incorporate more direct torsion angle information into the structure calculation. In addition, while extraction of the F-rates constitutes a linear task, in the case of nOe information, both of the involved protons have to be identified, thus increasing the complexityof the process. 2.1.6 Molecules under investigation: The 14-ntand the 30-nt RNA The 14-nt RNA (Figure 6A) was selected as a model compound to evaluate the accuracy of X angle determination from /-'DocSA since it is conformationally rigid and contains both canonical stem regions with a low divergence in X and a non-canonical cUUCGg tetraloop, exhibiting a broader distribution of angles. In addition, the tetraloop comprises an unusual U:Gsn, while all other residues adopt the ami conformation. A B U7 C8 U6 C16 A C 16 C 14 ----------G ----- G9 I0 C5-G A 4 - U11 U ? -- G18 A12 U9 C 3 -G12 U11- A2g G10 C2 1 G2 C13 GI- C m G1 C14 5' 9 cG - C 22 3 4 3' - G26 A- C3 _ G 2 8 G 2 - U*; G 1 - C30 5' Figure 6: Priny shoe inbx, satine and seorndarys uaum ef the 14-nt ( unaM oEs bigmy 45 3' and dx 30-nt RNA (B). 13 Q N lded eske am Chapter2: F(HCN)-Experiment Autocorrelated relaxation rates demonstrate that all residues but for the base of U7 in the loop are rigid at the temperature of 298K, at which the experiments have been conducted (see Chapter 3). Homonuclear 3J coupling constants indicate that the ribose moieties of all residues are fixed in one conformation. Although there is no structure available of the 14-nt RNA to date, the structure of cUUCGg-tetraloops has been consistently characterized by both NMR [9] and X-ray crystallography [10]. The 30-nt RNA (Figure 6B; PDB entry 1RFR) consists of two canonical A-form stem regions connected by three pyrinidine mismatch base pairs (U:U, QU, U:U) and an uCACGg tetraloop, which has been shown by NMR [11] to adopt a structure similar to the one of the cUUCGg tetraloop. The loop contains an unusual CG base pair. As in the 14-nt RNA, all residues are rigid at the measurement temperature (310K), except for residue A15 in the loop. 46 . _ . . . Chapter 2: F(HCi-Experiment 2.2 METHODS AND MATERIAL 2.2.1 Sample preparation The uniformly 3 C, 5N labeled 14-nt RNA (5'-PO4-GGCACUUCGGUGCG3'; bold residues constitute the loop) was purchased from Silantes GmbH (Miinchen, D). The concentration of the NMR sample was 0.7mM in 20mM KH 2PO 4/K 2 HPO4 , pH6.4, 0.4mM EDTA and 10% v/v D 2 0. The 30-nt selectively RNA 13 C,15 N (5'- PO4 -GGCACUCUGGUAUCACGGUACCUUUGUGUG3'), which is labeled in the G and C residues, was synthesized by Jens W6hnert by n /t transcription with T7-RNA polymerase with a linearized plasmid DNA as template and purified as described previously [12]. Unlabeled rNTPs were purchased from SIGMA (Taufkirchen, D); labeled nucleotides were obtained from Silantes GmbH (MUinchen,D). The final concentration of the NMR sample was 1.2mM in 10mM KH2 PO 4/K 2 HPO 4 , pH6.2 with 40mM KC, 0.2mM EDTA and 99.99%v/v D20. 2.2.2 NMR spectroscopy 2.2.2.1 F(HCN)-experiment The NMR data were collected on a Bruker Avance 600 MHz spectrometer equipped with a 5mm 'H{i 3 G/l5 N} Z-Grad TXI CryoProbeT, an AV 700 MHz UtraShield 5mm 1H{ 3c/ 15 T instrument equipped with a N} Z-Grad TXI probe, an AV 800MHz spectrometer with a H{' 3C/ 5 N} Z-Grad TXI CryoProbeT and an AV 900 MHz spectrometer with a 5mm TX[ H{ 3C/ 15N} XYZ-Grad TX probe. The data were processed on a Silicon Graphics computer (Origin2000) using Bruker NMRSuite (XwinNMR 3.5 and TopSpinl.1) programs and analyzed in Felix2000 (msi). Measurements were carried out at 298K for the 14-nt and 310K for the 30-nt RNA. The experiments recorded for the different molecules are summarized in Table 1. The sequences are given in the Appendix (Section A2.1). 47 (HCN) pulse Chapter 2: F(HC 2nd Molecule Experiment Field Strngth nucleu Number of M SW ppm] s Scans complex Plt ref cross t1 t2 600MHz 15N 15ms 40 64 1024 128 1024 700MHz 15N 15ms 20ms 15ms 5ms lOms 15ms 20mis 30ms 40ms 40 40 4 4 4 4 4 4 4 16 16 32 - 512 512 1024 512 512 512 512 256 256 100 100 42 30 30 30 30 30 30 1024 1024 1024 1024 1024 1024 1024 1024 1024 15N 13C F(HGiICr) 14-nt RNA 50ns 4 600MH-z 1 5N 15ms 40 64 1024 128 1024 700MHz 15N 15ms 40 16 512 100 1024 rF(H2' CQN) 600MHz 13C lOmns 7 128 1024 50 1024 rFI'GCi'N) 700MHz 13C 5mis lOms 15ms 6 6 6 6 - 1024 1024 1024 1024 32 32 32 32 1024 1024 1024 1024 6 6 6 16 1024 1024 1024 32 32 38 1024 1024 2048 5 5 32 32 1024 1024 32 32 2048 2048 F(H6/8C6/8N) 30-nt ~20ms RNA F(-6/8C6/8N) 900MHz 13C 30mns 40ms 5mns 800MHz 700MHz 13C 13C 5ms 5ms Table 1: 7(HC)-expamc 2.2.2.2 -Experiment arnia ot onide 14-r and de 30-ntRNA. J(C,H) coupling constants 3J(C2, ,H,) 4 and 3 J(C6/,,H ,) 8 1 coupling constants have been determined using the pulse sequence given in ref. [5]; experimental parameters were taken from the reference. The spectra were obtained on an AV 700 MHz UltraShield T instrument equipped with a 5mm H{1 3C/1 5 N} Z-Grad TXI probe with 16 (64) transients in both the reference and the cross experiment for the 14-nt RNA (30nt RNA). The evolution delay coupling constant was 47.6ms. The carbon carrier was set to 89ppm.L The spectral width in the carbon dimension was 20ppm. 200 (128) increments were acquired in the indirect dimension for the 14-nt (30-nt RNA). 2.2.2.3 Atocorrelated relaxation rates Autocorrelated relaxation parameters (R1 , R2 and the hetnOe) for C1 , and C 6/C have been determined as described in detail in Chapter 3. For the 14-nt RNA, rc has been extracted from a 48 Chapter2: F(HCN)-Experiment detailed model-free analysis, while in the case of the 30-nt RNA, no extensive data analysis was carried out at 310K and xc was obtained from the averaged R 2 /R 1 ratios as described in Chapter 3. 2.2.3 F-rate calculation All theoretical cross-correlated relaxation rates have been calculated analogous to Eq. (1). For the 14nt and the 30-nt RNA rotational correlation times c of 1.9ns and 4.1ns have been applied, as determined from the measurement of autocorrelated relaxation rates (see Chapter 3). The CS-tensor values and orientations as well as the lengths of the respective dipole-dipole vectors used in the different cases are summarized in the Appendix (Table A1). All r(X) correlations involving the 1 5N CS-tensor of N1 and N9 have been determined using C++ programming language. The coordinates of the 15N CS-tensor components and the CH vectors were obtained from a set of modified mononucleotides rotated around the angle in the program INSIGHT II. These coordinates were then put into a C++ program in order to calculate F. For c-', S' A c 6D8,CSAN/9 and rH6'8CSA9C618, coordinatefile independentcalculationswere carried out using C++ programming language. A detailed description of the parameterization procedure is given in the Appendix (Section A2.2).In the case of rF' iclsX only the orientation of the tensor components in respect to the C-H r . bond is known. The maximal possible value of o rH'DC cl has been calculatedby rotating the tensor around the C.-H r bond using the program Mathematica. 2.2.4 RNA structure calculation Structure calculations on the 30-nt RNA have been carried out by Oliver Ohlenschliger at the IMB in Jena using the program CYANA [13]. The calculations comprised 937 upper distance restraints obtained from nOe intensities, 735 of which were either intraresidual distances involving the I- 5 ,/H5 ,, or interresidual restraints, the rest were restraints ensuring the circular ribose structure and hydrogen bonds distances. In addition, 212 lower distance constraints were incorporated for ribose ring closure and the hydrogen bonds for the base pairs within the stem-regions (1-13; 18-30). Furthermore, 118 angle constraints were incorporated: The backbone angles a and ( were constrained according to 49 Chapter 2: F(HC)-Experiment phosphorous chemical shifts; 6, v1 and v2 were constrained to fulfill the ribose pucker requirements. Xangle constraints were directly incorporated as angles with a variance of + 10° . All up to 4 possible X angles obtained from the degenerate F(X) parameterization were included resulting in a total of 38 X restraints for 10 residues. Out of the 200 structures calculated, the 40 best one (with a target function lower than 0.47A) were selected. 50 Chapter 2: F(HCN)-Experiment 2.3 RESULTS 2.3.1 The quantitative F(HCN)-experiment 2.3.1.1 Pulse sequence The pulse sequence and the experimental parameters of the quantitative F(HCN)-experiment are shown in Figure 7. A quantitative approach has been selected, in which F'cDCSA is obtained from the relative intensity of the same cross peak in two subspectra. The experiment is a modified HCN-experiment [14-19]. The magnetization transfer is given in detail below the pulse sequence (Figure 7). CN-double- and zero-quantum coherence is excited at time point a and allowed to evolve for a variable delay rM under the influence of r ooNcSAinto one term, which is b-modulated h by the F-rate (4HC/F, NpsA modulated term (2CNsin(HDcDcsA *,)), and into a second sin- at tme point b [20]. Two experiments are recorded, the *rM)) reference experiment, in which the tush-modulated operator is transferred back and the cross experiment, in which the sinrmodulated operator is achieved in an at-and-hik operator is selected. While selection of the reference manner, the specified phases (caption of Figure 7) have to be shifted and an additional proton-carbon recoupling period has to be introduced in the cross experiment. Furthermore, a proton 90 ° pulse is applied after remove any operators involving protons. HDCSAN TM in the cross experiment in order to can be determined from the peak intensities in the two experiments according to Eq. (3). (3) r DDCSA= tanh -( nsf cro HC'N~~~~~~ In this, nsd and sd M crossI ref are the number of transients and pr and 1- are the peak intensities in the reference and cross experiment, respectively. In principle the F(HCN)-experiment 1 simultaneously, thus obtaining can be applied to the base and the ribose moiety CSA .Hr CrN/9 ],DS and HD6DI'CSAN1/9 at the same time. However, sensitivity is improved by running two separate experiments, since the HG and CN-transfer delays differ for the ribose and for the base moiety. In addition, the carbon carrier frequency can be set on resonance, when running both experiments separately. 51 Chapter 2: F(HCN-Experiment TROSY ~~~~~~~~~~~T T. t T. t cross ~ ~~~ .... ~ _.~ ~' ~ ~ ~~=2T -A rf+................... I~~~~~ I * ,',-....~Y.................. cross~~~~~~~~~~~'" 2 ' = 2T . ................... ' ........ ;, ' ,"; . ... ' ...';... I Y ..... I 'H I WFII 15 N G 1 + rf cross .... ~ : .~~ : I G2 .I : 96 AIT-A ~ (P7 I 2CYH.S(F¶M) I ~~~~~~~~~~~~~~~~~~~ C2'IC5 : ~~~~ PS ~~~~~~~~93 (Ps a &2 22 (N (Ps T-AATIAEAI 2C.N.S(Pr-m) i~tiA 4 IC~ I4 G4 G 4 &G I4 b crs , " Y I T2 cross~~ IC~srM Hy 2 2- I .I. 1 2C.N.S(FrM) 1221IiA *~~~~~~~~~~~~~~~~ II :* 2 I ='.2Tii 13CTII (Pi cross I I T cross 2 2 1 I HAsFTM) GARPI :~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~ IefcrosszIyH ' 6 IC~SrM MH I I I GARPI G7 I I) lyll '- Magnetization Transfer ref 4CYNYHzC(F¶M) H2CI~c Figur 7' Qritatiw -CNH I(HCN)-expefrnen 4CYNzHzc(rTM)1JCH 2CYH.C(rirM) HACFTM) nNH H,N Narow and ide bars aconpr sto 90 and 180 degme pulses, respeatiy Sdewpulses andgradi are iit by semi-e.gses.Thedefat pulsephe is x. he ni e and e cras ex t aresnm zed in oe pulseseque7e sdm For nth, e rp nn phses 3, (p4am set to x, is set to y and te haed 180°0 pulselalxdd fis appliedonprm. In te oas ex nn ples , epare set to: (s is set tox andithe hadsd 900° and 180° pulses lad cmss areappliedA sletie off-o t ptlseon C2 orCs drg cam am otnt tine enicalshf edaim is shom in gy A aq onSparanmet for r o,cDC (rH,C "Ja . A419/is e 1 tto 1/(2 9 t'A 6/ IC',NII1 H8C618,Nl/ 12*1~ 1 andsetto3.2ns (2.4n); T=1/(2*Jvc) is38ns (32r); r i the m set to 89ppm(141pp) andthe rtgenet Ci'/CC&: 1.77rs Q3 rasing at 158ppm At , °DD ;CS 600MHz, raxat petc Thecaa n iet s sd elaepulses mre set asfdlos: pulse [21]; Nl/N9.g: 1.7r IBURP2 imersionpulse [22]; C2 '/C 5. 512/1s Q3 pulse Waterfliphbzk (WFB): ln sr puse. Gradientas: Gil=lrns, -20Gonl; G2 =1rns,20Gonl; G3 =1rs, -25Gonl; 1 G4=500ps, -2.5Gon; Gs=lrrs, 22.5Gon ; G6 =1ns, 2Gnm; G7=ns, 10.05Gan1 . Phase cydinr (0-=x,(-x); (= 4y,4 (-y); q3=8x,8(-x)for he *e exmr ; 8 y,8(-y)fir the ass exp rmt (p4=16x,16(-x) in the e/m expemrn, 16y,16(-y) in te crss expeit =x,2(-x),x,(-x),2x,2(-x),2x,(-x),x,2(-x),x,(-x),2x,(-x),x,2(-x),2x,2(x),x,(-x),2x,(-x).Sates- TPPIphase disinition [23] in oi s tair by shiing phase =x,y Gradie ie selcion in 2is adiezdbyshifgpases (6=2x,2(-x) and q7=2(-y),2ytiher uith dangigthesign fG 6. Asynom GARP dling Magtizati [24] is sed to spss tramferpadmay in the *men TROSY.Eution of the GH TROSY her de salarmplingsduig acqisitn Magnetization Tnsfe ('ref) and the crss expe arnt 52 ('crass). C0sh is abnuted by 'c, sirnh by ' Chapter2: F(HCN)-Experiment Although the F(HCN)-experiment is shown as a three-dimensional sequence in Figure 7, it is not meant to run as such due to the time requirements for the cross experiments, where at least 256 transients have to be acquired for each time increment in the indirect dimensions. Instead, depending on the resonance dispersion, either the carbon or the nitrogen 2D plane or both have to be acquired. It has to be noted that 3C is preferable to '5 N chemical shift evolution, since the latter takes places in a real time, while the former occurs in a constant time period. Real time chemical shift evolution in general constitutes an additional time interval in the pulse sequence, during which in this specific case the favorable TROSY-effect is averaged out by the 180° proton pulse.The total CN-transfer delay (2T) constitute the longest period in the pulse sequence (62 or 76ms). In this time interval, relaxation of the carbon transversal magnetization due to CDCSA cross-correlation with the directly bound proton is significant[14, 19]. Depending on the spin-state of the proton, the dipolar and the CSA component of the relaxation mechanism counteract (TROSY-effect;[25D)or add up (anti-TROSY-effect). In order to minimize signal loss during 2T, the slowly relaxing CH TROSY component has to be maintained. The evolution of the TROSY (+) and the anti-TROSYcomponent (-) are shown in Figure 7. While 180° pulses on carbon do not affect the TROSY evolution ('cDCSA ), since they switch both carbon operators, the TROSY and the anti-TROSY component are interchanged by proton 180° pulses. The necessity to recouple protons in the cross experiment results in evolution of the anti-TROSY component for a period A, while in the reference experiment the TROSY component evolves for the whole delay 2T. The loss in signal intensity due to this additional relaxation effect in the cross experiment as compared to the reference experiment has been estimated from the of the calculation s6/8,N1/9 to be less than 1%. In this calculation, carbon CS-tensor values determined by Stueber et al. [8], a field strength of 600MH-zand a ; of 1.9ns and 4.1ns for the 14-nt and the 30-nt RNA, respectively, have been used. For C1 ,, this contribution is even smaller than for the base moiety, since the CSA of aliphatic carbons is significantly smaller than the CSA of aromatic ones. Therefore, this differential relaxation effect in the reference and the cross experiment has been neglected altogether. The reference and the cross spectra of a 13C 2D-F(HCN) applied to the ribose moiety of the 14-nt RNA are shown in Figure 8. The experiment has been run at a 700MHz spectrometer within about 15h. The experimental sensitivity is sufficient to yield an error in the resulting F-rates of 0.1Hz on average. 53 Chapter 2: F(HCN)-Experiment The relaxation delay rMhas been optimized for maximum signal intensity in the less sensitive cross experiment, which picks up the srimodulated proportional to sirf£*ru) cross operator. During TM, signal build-up is counteracted by signal loss due to autocorrelated relaxation of the CN- double- and zero-quantum coherence. A B [ppm] U7. - c8 13 [ppm] - c -87 13 c -87 -88 -88 0 a -89 -89 -90 -90 L. G12 A4."eC14 G2 S G9 6.0 U11 · eC5 C3 C13 OS * I 5.0 4.5 4.0 'H -91 * -92 U6 5.5 GlO -91 G10 6.0 [ppm] -92 5.5 5.0 4.5 4.0 'H [ppm] Figure 8: -C 2D-(HCN)-spectra ofthe ribosenietz f the 14-nt RNA. (A) ROfem exennmng(B) aurs expem-m the semiisdty in the tzeo expernn. he spectrahae been rmmd on a 700MHz speamvnrter,rM wtsset to 15nr;the nmm epXennr 'tws ! *aiwth 32,the Resonaxr assignrn rsseemnv aregin D-slices drmgb the reswme ofGl O denmtrate wth 1024 tramiens. For the ribose moiety, cross peak intensities of representative residues (Figure 9) show that a rMof 20 to 30ms is optimal for both the 14-nt and the 30-nt RNA. Due to the larger chemical shift anisotropy of the aromatic compared to the aliphatic carbons, which constitutes the main difference between the two moieties, optimal evolution delays for the 1F(HCN-experiment applied to the base are expected to be of the same order or slightly shorter. 54 Chapter 2: F(HCN)-Experinment 14-nt RNA 30-nt RNA "7 h(d - .Fa 0 , G1 0 041 043 -0 § 0.03 044 .T "~ , ~ .. t - r 0.05 i 0 --t~~~~~~~~ C14 0.ILCD 75G..... C,4 4tM [S] TM[S] inte 1(HCN)cross ex mnta o e Figure 9:Peakieoiti i d dn ffe edu im delayrMf seareortos arnd tpek ierites arisefmpncsze or W e ri0e nrietyfor the 14-nt(left)arndthe30-ntRNA (ri. Pacsitizw sig orthef -rates.Data hasben arat 700MHz ihzb 512 (256) traraie foreab tr imrntfora rm fC5 to 30n (40 to 50rrOns) for tdxe14-ntand 1024 trarmients fr all zm ddasfrte azewraged noiseleze 30-ntRNA. The er rs hae ken takenfimt 2.3.1.2 Derivation of F(X) parameterizations For all F-rates, F(X) parameterization curves had to be derived. These (X) parameterizations follow Eq. (1). Hence, isotropic diffusion as well as the absence of internal motion (S2=1) is assumed. CS-tensor values and orientations reported for adenosine, cytosine, 2'-deoxythymine and dihydroguanosine in the solid state [8] are used. The N1 CS-tensor from 2'-deoxythymnine has been used for uridine, because no tensor for this nucleoside is available to date. The global rotational correlation time tc has been obtained from autocorrelated relaxation rates (R1, R2, hetnOe; see Section 2.2.2.3 and Chapter 3). TcDDCSA ,H,.N (*) __ _A__ Adenine Cytosine Guanine Uddine = = 10_ o [Alcos(X)+ A2 cos(2*) + A3] A A2 -5.933 -7.137 -6.828 -6.860 0.332 -2.123 1.265 -2.908 Table 2: Famerexparon of de depo ef tn' Bo= rmgcfiddsmt in Tesk r Hicl, 9 nZfor 55 A3 3.338 4.059 3.271 2.917 d7e mdeaides. rc=ozeralrtatnl wndation Chapter2: F(HCN)-Experiment In the case of r , the parameterization is a straightforward application of Eq. (1), which IooC1 has been expanded into the nucleotide specific Fourier series shown in Table 2 in order to facilitate the angular interpretation of the F-rate. These parameterizations require only to incorporate the rotational correlation time of the investigated molecule and the magnetic field strength of the spectrometer. Nucleotide specific F(X) correlations for the 14-nt RNA with a correlation time of 1.9ns, are shown in Figure 10. For all nucleotides, the slope of the F(X) correlations is steep in the most Figure 2) combined with a frequently adopted range of the most populated anti region (180-210°; sign change, offering a sensitive parameter for X. In the most populated swnregion, however, the parameterization curves are flat, indicating that angle determination will be less precise in this region. At closer inspection, it becomes apparent that the results of the F(H-CN)-experiment are not as easy to interpret as expected. A more thorough analysis reveals that in addition to F ,cSA dipole-dipole, CSA contribution has to be taken into account, namely Fr Adenosine N 6 I 1.5 I 5 4-R 0.5 7 2.5 6 1.5 5 0.5 4om 3 -0.5 -1.5 1 -1.5 -2.5 0 3610 -2.5 90 180 270 3 Q_ -0.5 2 0 2 LL: 0 90 Cytosine 2.5 6 Ir 1.5 5 ? I A -0.5 I 4om 2.5 6 1.5 5 -1.5 1 -1.5 -2.5 0 -2.5 180 x, II] Figur 10:Nudect spea r idis 270 7 4.m o~ .. 0.5 Qi. -0.5 QO~ .0.5 3 2 90 360 3 2 1 0 90 swsryhon 180 270 0 360 Xo1 CsA (,) parane ionaes fr the 14-nt RNA at 600MHz. The ane in the ag riboas subuit [2] are shen in gny ThenMst also in 0 36 0 8 3.5 7 0 270 8 3.5 0.5 0;2 180 1 [] X [0] pims 8 3.5 7 2.5 'CSA Guanosine 8 3.5 asecond zamhizgbibW 56 .. .... - . a anle gom ite an andfordx Chapter2: F(HCN)-Experiment Since rFoo cSA and "HCN rF'HN ,CSA ,C arise from interactions involving the same operators, q, Hz and N, (for the former [[2qHz,[Nz,p]]; for the latter. [[2NzHz,[q,p], they cannot be separated experimentally. In addition, the evolution of both cross-correlation rates results in the same cross operator. For the ribose moiety (Figure 11A), rFDD,CSA is small due to the small anisotropy of the C, CS-tensor, which is around 30ppm in the C3-zo and about 60ppm in the C2-endoconformation [26]. Although no complete orientational information can be obtained for this tensor to date, the approximate contribution of to the overall rate has been calculated from the C1, CS- rNJ,9,cl tensor values and their projection angles on the C1-H1 bond provided in ref. [14]. Since this tensor displays an anisotropy of around 60ppm it can be used to judge the maximal possible contribution of FD,IcSA' For the 14-nt and the 30-nt RNA with a rotational correlation, time of 1.9ns and 4.1ns the maximal contribution of rFJ'DCIsA, amounts to only 0.06 and 0.12Hz, respectively.This small contribution has been neglected in the following analysis. OH .v-vv.r OH A l-~ ~~DD ~ .CS ,c (4 aMTH alr~~~~~' Figur 11: (iHt/N1/9c/8(B 9C618 B .CSsctrAw f"the (B).The '3C 3 SA and the leftdN- For the base moiety (Figure 1lB), nucleotide specific rD' based on 13 C H oraeg / 9 C618 values have been calculated CS-tensor values taken from Stueber et al. [8]. The results are shown in Table 3 in comparison to fD,CSA I6/sCf6/8N1/9 -rts r'o "'i~rsieDD.A Since the two F-rates are of similar size, neglected. 57 H6I8NI 9 C6/8 cannot be Chapter 2: r(HCG-Experiment DD,CSA r H6/8N1/9,C6/8 [Hz] -0.60 -0.76 -0.59 -0.78 Adenine Cyt:idine Guanine Udine Table3: 3: F, r'DD, CSA 6 I 8 Table n68Nl19,C618 6 a DD,CSA H6/8C6/8,N11/9 [Hz] -0.91 -0.45 -1.46 -0.17 fr for d''e dA 10E~ dr D,CS,4 FI6/8N1/9 "n618C618,Nl<9 fian a "N CS-15NaMi badOni13C 3CagsNC-edTo$ ~ n~"" Studeret aL [8]for the 14-ntRNA at 600MHz. If both r'HpDcSAand rFHDNDcsA have to be taken into account, the evolution of the operators during TM differs from the one discussed in Figure 7 in the presence of just one cross-correlation. In this case, the reference (Eq. (4)) as well as the cross operator (Eq.(5)) evolve with the product of the two F-rates. 4H AI h( 4HzCyNpoh( (4) rDD (5) c DD ,CSA ,N,CSA r)) csh(f HN,C ) M) sA *rm) sinh(DD'cSA*) ~4CNsinhb(F The ratio of the cross peak intensities in the reference and the cross experiment can be simplified to Eq. (6): I cross_sin[(FHCN +FHN,C )*T ] (0/ Irf For small values of lim(cosh(x))=l TM and cosh[(FHCN rHNC )*T] FHCJ - and FHDS i-rates of similar size, lim(sinh(x))=x and apply. In this case, Eq. (6) can be rearranged to Eq. (7): X-0O Icross (7) Iref = (FHC,N + HN,C) * TM Using a typical TM value of 0.02s, this approximation is accurate within a 1% error margin for (-S HCN "NDcS ) values of up to 7, which correspond to a correlation time of about 8ns for guanosine, 1ins for uridine, and 22ns for both adenosine and cytosine. Hence, for RNA-molecules which is the of up to about double the size of the 30-nt RNA, Eq. (7) can be used to obtain F-hbase, 58 Chapter2: F(HCN)-Experiment sum of the cross-correlated relaxation rates, FJCDNSA +-vl s .NC -hse parameterizations for the different nucleotides are summarized in Table 4. 7 Ftse=10 BorCA4 A4 Adenine -5.105 Cytid&ne -4.057 Guanine Udine -6.922 -3.206 Table 4:Paramwnzation r F base Consequently, the ratio of r cs and F-ase yields the c and B independent F-ratio() relations given in Table 5. T - ratio () = 107 [Alcos(*) + A2 cos( 2Z) + A3 ] Adenine Al -0.065 A2 1.162 A3 -0.654 Cytidine Guanine 0.523 -0.183 1.759 0.986 1.000 -0.473 Uddine 0.907 2.140 -0.910 Table5: Fner epamnin fhdepdgf he F-ra onfor th difr e m 2.3.1.3 Determination of X from rH ,csA1 -D,CSA FHDDcSA /9-rates have been extracted from the peak intensities in the cross and the reference spectra of the F(HCN-experiment as described in Eq. (7). The measured F4D"cIslc -rates and resulting X angles for the 14-nt RNA are listed in Table 6 together with the reference angles from the crystal structure. Also given are angles extracted from the measurement of 3J(C,) coupling constants. The precision of F-rate determination is 0.1Hz as obtained from the mean deviation of the F-rates for all residues from multiple measurements at different field strengths and different relaxation delays rM(see Materials and Methods). 59 Chapter 2: F(HCN)-Experiment r DD,CSA 1Hl'CI',NI/ Residu , 9 [H][Hz] Residue F-base " Hcr DSAN9 F-tio X[ I 3 J(C,H) Refemrence G1 G2 C3 0.67 + 0.04 0.14 _+0.01 -1.16 + 0.18 -0.99 + 0.16 -0.66 + 0.00 203 + 1 203 + 1 192 + 4 201 + 1 192 + 2 - 194.8 + 4.4 194.8 + 4.4 198.4 + 3.1 A4 0.44 + 0.01 -1.30 + 0.11 205 + 1 204 + 1 198.5 + 1.5 198.2 + 3.5 C5 U6 U7 C8 G9 0.32 + 0.07 -0.29* -0.99 + 0.11 -1.03 +0.08 -1.64 +0.35 -0.68 -0.56 -0.35 -1.00 -1.92 + 0.05 + 0.04 + 0.10 + 0.00 + 0.20 200 + 1 202 212 + 2 221 + 2 60 + 8 197 + 2 205 + 1 240 + 9 226 + 3 60 + 7 191 + 8 196.5 + 4.5 217.5 + 9.5 210.5 + 6.5 93.5 + 4.5 197.9 211 223 202.6 58.7 G10 1.00 +0.11 -1.09 + 0.08 198 + 2 184 + 4 215.5 + 13.5 198.3 Ull 0.29 -0.30 + 0.04 194 187 + 1 - 198.2 + 3.0 G12 C13 0.53 +0.04 0.21 +0.04 -1.10 + 0.04 -0.80 + 0.15 206 + 1 202 + 1 198 + 2 200 + 1 192 + 4 189.5 + 3.5 194.8 + 4.4 198.4 + 3.1 C14 -0.55 +0.08 -0.85+ 0.01 212 _+2 216 _+2 198 + 5 198.4 + 4.4 6.8 13.1 7.2 14.7 8.3 9.7 * p DDCSA RMSD DIN/,r _,_csA 6.8 13.1 F-Mtio 3J(GH) [0] ' ° c Table 6: rH~I'CI',N s 19 xang and F-baseforthe 14-nt RNA. HI1',N,/ 14.7 rsultingfromtheaml)sis ofalone DrFo,1/9 andfirm the ratio of the to Frates are cpared to the arns fiom the cstal striazure(oldm deatd Referx) andfrom the at 600 andat Fratesfirn nasens interpmtation f3J(CH) ortplingcwtants (almn denoed'3J(QH)). Theazeraged ty pecspcKarplus700MHz aregiwn 3J(C,H)axling constants haze n demein and analyzedby a refir mdeide. relationas describedpziosly[4-6].Aeragedanglesfimtheanalsis of3J(C2/4,Hl)and 3(C6/8,H1) aregi E rro for TM edution pmios and dffrent rmg fields(see the F-rateshae bn caladated firn mltiple nraswrnts at diffemvnt differns heeen angle Materialsand Metdls sectio*; ers for coling constantdenizedX anles hawebeentaken fim thedx detminationfltyn3J(C2/4,Hl)andfom 3J(C6/8,Hl). For both F-rates and J-couplings, only the X angles closest to the reference values have been extracted from the degenerate parameterization curves. The agreement between the X angles derived N'IN/9and the reference angles from the X-ray structure, RMSDrF(CHN)/x-ray, is 7.2 °. from 'r' D-Do,CSA This agreement compares to the one between the reference angles and X angles obtained from the analysis of (RMSD, 3 J(C2q/,H r) 4 1 J(C ,H) IX-ray = and 9.70). 3J(C6/ ,H r) 8 1 coupling constants, which are also given in Table 6 The consent between the J-coupling and the cross-correlated relaxation derived X anglesis slightlyworse (RMSD, J(c H)/r(HCN) = 13.1°). For cross-correlated relaxation rates as well as coupling constants, the deviations from the reference angles are significantly smaller in the stem-regions 60 (RMSDr(CHN)xray (stem)=6.0°; Chapter2: r(HCN)-Experiment RMSD3 J(C H)/X-ray (RMSDr(CHN)/X-ray (stem)=4.4°) than in the non-canonical loop region (loop)=9.9°; RMSDJ(c, H) / X-ray (loop) =17.1°). A major contributor to the high RMSD of the coupling constants as compared to the F-rates in the loop region is residue G9, which is in the sn conformation. Whereas X is 58.7 ° in the crystal structure and 60 ° from the analysis of cross-correlated relaxation rates, the coupling constants result in 93.5 °. In contrast to differences in precision for different secondary structure elements, no base type specific differences can be determined within the limited number of investigated sites. 2.3.1.4 Determination of from F-matio F-ase values of the 14-nt RNA are listed in Table 6. In Figure 12, experimental F-ratio values are plotted against the reference angles together with the theoretical parameterizations of the individual nucleotides. The X angles resulting from F-ratio are also given in Table 6. The overall agreement between these and reference angles is RMSDr,, x.ay= determination is the same as from the analysis of rHD'c,cl determination methods proposed here is RMSDra./x,, 8.3 ° . Hence, the precision in angle alone. The agreement of the two angle = 6.3 ° . As for rDDCSA the precision is higher for the stem residues (RMSDrraio/ xray(stem) =6.3° ) as for the ones in the loop (RMSDFratio/X-ray(loop)=11.9°). For both methods, Xof G9'Ynis 60°, since the measured value exceed the values in the parameterization curve and 60 ° is the angle in the syn region with the maximal rate. However, subtraction of the error of the measurement yields values within the parameterization. Figure 13 shows correlations of the X angles derived from r'oocsA alone and from F-ratio compared to the reference angles. Although there are differences in the deviations from the reference angles, no systematic differences can be detected between the two techniques. 61 Chapter 2: F(HC)-Experiment 3.5 2.5 1.5 2 .- ' 0.5 -0.5 -1.5 0 180 90 270 360 Xl Figure 12:Exprna paraeatm. F-ratio pkateagist themfwe al andthoica Fratid,) i fr the 14-ntRNA F-ratio " 250 aa ADU 230 230 b o 0 _ 210 f 210 190 190 190 170 170 170 190 210 230 250 170 190 Xref[] Figume13: Xargz dtdfiTn Lop residuesare lll by bces. X e 210 250 230 Xref ] I 9,cl, (lft) andF-ratio (riit) twpandto ew an for G1 arenimsis sime rHF 62 9,C, = not be for th 14nt RNA. 'vfr esid Chapter2: F(HCN)-Experiment 2.3.1.5 The N CS-tensor in solution from F-base Figure 14 shows F-base obtained for the 14-nt as well as the 30-nt RNA sorted by base type compared to the theoretical F-basevalues. -0.5 -1.0 ± -1.5 -2.0 8 . (cI c ct *+ + 14-nt RNA 0.0 ] . + ½ + - . --- 4 3 5 -2.5 A Q 1 W I' 4A I39;i 1 - 2 9 1012 C G 6 7 11 U 30-nt RNA 0.0 -1.0 N -2.0 4~~ 'T' I: -3.0 co, Q -4.0 -5.0 -6.0 -7.0 374162122301 5 -3 2 9 10182 5 7 1416212230.1 2 9 10182628 . G C Figue 14: Expenntal and theoreia ults the (HCN)-exnt appliedto the base nrety ofthe 14-nt (to) and the 30-nt RNA (botorr sortedby base type Gddated F-base luesare indicatl by dashedhorizonta1lires. Lop residuaes are laid zdthbocesand hghlightedby greyshading For the sdectidy laded 30-nt RNA, F-basezaluesare gizn onlyfor the 13C1SN lalde guansi ad cytosimresids. The datafor the 14-nt RNA has beenobtairndat 600MHz, the onefor the 30-ntRNA at 800MHz. 63 Chapter 2: F(HCN)-Experiment Since -baseis not dependent on the conformation around X,comparison to the theoreticalvalues allows to obtain information about the characteristics of the N 11 9 and the C6/8 CS-tensor in oligonucleotides in solution. Unfortunately, no individual information on either tensor can be obtained, but only their combined effect on F-base can be interpreted. From this data, the following conclusions can be drawn about the CS-tensors in the bases of RNA: (i) They are base type specific. In the stem regions, all the adenosine, cytosine, guanosine and uridine residues of the 14-nt RNA and the cytosine residues of the 30-nt RNA exhibit similar values for each base type. These canonical F-base values are, however, in general not in agreement with the theoretical F-basevalues. Apart from the cytosines in the 30-nt RNA and U7 of the 14-nt RNA, the theoretical values are in better agreement with the loop-residues than the canonical stem residues. (i) They are correlated to the theoretical values. The relative size of the stem adenosine, cytosine and uridine residues in both molecules matches the relative size of the theoretical values. For guanosine, the theoretical value matches the value for G9 in the syn conformation. (iii) They are conformation dependent. All the loop residues (except for U17of the 14-nt RNA and C16 of the 30-nt RNA) exhibit cross-correlation rates, which are significantly different from the ones in the stem-regions. The first observation is intuitive, since the nuclei are surrounded by a different chemical environment in the different nucleobases, and in agreement with earlier observations [8]. The failure of the theoretical F-basevalues to reproduce the experimental values of canonical residues is contrary to the better fit of the experimental X angles in the canonical as compared to the loop regions. The second observation is expected, since CS-tensors of the same compound environments in different should exhibit at least similar characteristics. The last result concerning the conformational dependence of CS-tensors is still subject to debate in the scientific community. 64 Chapter 2: F(HCN-Experiment 2.3.1.6 Transfer to larger systems The cross and the reference spectrum of the F(HCN)-experiment applied to the 30-nt RNA (Figure 6B) are shown in Figure 15. The spectra were obtained at a 900MHz spectrometer using 1024 transients per t 1-increment. A B [ppm] [ppnm] 13c 13 -nC 87 -87 88 -88 89 7 VW G2 G28 C721 0o0 -:C21 G1 0 . . ..I -91 C30 *C5 ....... 6.0 C A * C14 7- u V 0 C22 G17 . -89 I 91 2, C22 -92 -92 I I 5.5 5.0 I I . ' 4.5 4.0 1H [ppm] I . I I.... I 6.0 . I ..... ' I 5.5 . . . . . I . 5.0 . . . ' I.... . 4.5 'H Figure 15: (HCN)-spearaf the30-nt RNA. (A) RqOfr exp'n . . I . . 4.0 [ppm] (B) arss cpeinm Resonanxassigma are giwn The spectrahawebeen aEd on a 900MHz spea xte rM ms set to 5ns; the ,b expe pme Usdai m 32, the crss expenn teih 1024 trarsient; The oerall duration the ttm expent r s abwt 15 hotins. FJif4CSA th F-base and the extracted X angles are given in Table 7 together with X values derived from the analysis of 3J(C,H) coupling constants and the reference angles from the NMR-structure [11]. The accuracy of X angle determination is 11 when derived from rHD4 oc CWs alone and slightly better (RMSDF ratio/NMR= 8.6) when the F-ratio is used. Angle values obtained from 3J(C,H) coupling constants are in good agreement with both the reference as well as the cross-correlated relaxation derived X angles. 65 Chapter2: F(HCN)-Experiment Residue - Fbs ]',DD CSA '~H1/9,F [Hz] [N1/9 Hz] [Hz] C -3.95 -3.06 -2.59 -2.56 -2.74 + + + + + -4.29 + 0.28 0.03 0.22 0.04 0.34 0.33 FH DD,CSA 208 + 190 + 189 + 212 + FJ(CH) I'-d0 205 + 191 + 189 + 212 + - G1 G2 C3 C5 C7 G9 1.17 3.21 3.57 -1.59 - G10 - -5.17 + 0.25 C14 C16 -2.05 - -3.99 + 0.14 -3.07 + 0.16 G17 -1.91 - G18 - -2.27 +0.12 - - C21 2.43 -2.80 + 0.20 194 + 1 C22 3.38 -3.24 + 0.17 190 + 1 G26 G28 C30 0.75 -1.49 -5.98+ 0.17 - - -3.12 + 0.26 -2.93 + 0.80 210 + 1 211 + 1 rDH 'N1/9 ,CSA J(C,H) C/SA 215 + 1 211 + 1 - TZ) dest x anglesfor 13Q 15N lied F-baseand resdulting to the refer 194 + 4 194.5 + 4.5 191.5 + 4.5 201 + 9 209.5 + 2.5 193.6 + 204.3 + 201.1 + 206 + 198.7 + 195 + 0 196.7 + 1.5 197 + 4 202.5 + 10.5 201.6 + 2.2 197.8 + 4.9 angle is shozen Angle defatic 0.5 0.9 1.3 3 1.6 195 + 1 200 + 8 199.8 + 1.6 193 + 1 194 + 4 197.5 + 1.6 209 + 1 211 + 2 222.5 + 14.5 200 + 3 208 +4 196.8 + 0.9 193.2 + 0.7 211.1 + 1.5 1.4 8.7 11 7.6 8.6 1.4 8.7 MR- structure 65.2 + 1.1 7.6 7.5 ancire an cytcineresidues f the 30-ntRNA wnTamred to the X anglesfiman the NMR-struawre [11] andfroirm the intpretation sdution for 0 97 + 5 85 + F-rtio [0] 1 1 1 1 - p1DD CSA R SD Table 7. F 1 1 1 1 [ f 3J(QH)-capling constants.Ornly thed for the Frates zeerecaladated using thedx aweraged RMSD f O.1Hz as determirdfor thedx 14-nt RNA; deziationsfor 3J(QH)-.derizeda angle recalated from thedeziations fangl resultingfm dxthe analyisqfJ(C2/4,H1) and3J(C/8,Hl). 2.3.1.7 Incorporationof rD'cs' ,c, into RNA structure calculation In order to evaluate the structural relevance of the X angle restraints derived from r Dc Ac1 they were incorporated into a Distance Geometry/Simulated Annealing structure calculation in torsion angle space of the 30-nt RNA. The calculations were carried out by Oliver Ohlenschliger at the IMB in Jena, who had previously determined the structure of the 30-nt RNA by NMR [11]. For this structure calculation, an exceptionally large set of nOes has been used (- 27 nOes per residue), resulting in a very well defined structure (RMSD 0.67 A for all heavy atoms). For comparison, two calculations have been performed, one comprising only a minimal set of easily accessible nOe restraints (with the exception of nOes involving the H5 /H5,, protons, all intraresidual sugar-to-base and sugar-to-sugar nOes (225 in total) were removed) and a second one, in which the F-rate derived restraints were added. In this case, X angle restraints were directly 66 Chapter2: F(HCN-Experiment incorporated as angle values with a variation of 10 degrees. All possible angles from the F(X) parameterizations were considered. _FDD,CSA Cl 'H1'N1/9 +IFDDCS4 CVHI '11N119 Figure 16:Resultsf the CYANA sctme cadati on the30-ntRNA. A bxze Z ane di guxne midua,for uhicha r HICI',NI/9 DDclCsA cd be abta4 esdidtigfia*n dx stmcue aklation na whes(se tct). BdoezX ax c&isttims muigfine and Z ange retrnts fm fon a ?igS j 9 6tie and a ninmil set + stmut aldati ii the an3sis ef rFgD9csAI 9 . In boh caes, Z arl frn 1IC',NI/ a mil set nCe vudp te 40 stmirms thd louest taet Ysfirtan dx aalaoemaie of200stres areshon Inclusion of the r' oCsA1 9 derived X angle restraints results in a decrease of the mean RMSD from 6.9 ° to 2.6 ° for residues G2, C3, G5, G7, C14, C21, G28 and G30 (Figure 16). For G17, which is in the syn conformation, the nOe based structure calculation results in a X angle of 67.5°+ 3.8° . Upon incorporation of the F-rate derived X angle restraints, two X angles become possible, 42.8 ° and 79.6 ° , signifying that in this angle region, nOe and F-rate data are not sufficient to discriminate between the two possible angles derived from the F-rates. 67 Chapter2: F(HCN-Experiment 2.3.2 The quantitative F(H2'C2'N)-experiment 2.3.2.1 Pulse sequence (Figure 17), the first INEPT module is used to create In the quantitative F(H2'C2'N)-experiment C1 H 1,C.-antiphase magnetization. During the following delay T, magnetization is transferred from Q, simultaneously to both C2 , and N1 (pyrimidines) or N9 (purines). In addition, the H1 , operator is refocused during a delay A. At time point a, the double- and zero-quantum operator 4C,,,C 2,yNy has been During created. rH2%C25,sAN9 TM, is and active operator this evolves 2',.snh-HfC2',N1at time point ,C2,Nxsinh( *t, and 8H2,,zC 4C,,zC2,yNycosh ( r Doc25a 22'NII9 ' into b. In order to transfer the latter operator back in the cross experiment, H 2 , proton magnetization is refocused during an additional delay A subsequent to b, while the reference operator is transferred aot-and-li. cross ref Y 1H 2 ! 2 * qX, I| 3 I DIPSI-2 DIPSI-2 *'P.P2 22 (Ps 2LY' a A A b' l TI#tIA ~15N ''4`1~ O 2 9)6 I GARP A2I2 I? (p4 (P3 GG T| 2 IGARPI ' * : :G 3 A: Gz Magnetization Transfer : CH ref HYCH6-2CH H;94 I 2 C JCNH JCH 2.YH,.Zc(rTM) 4C..C 2.,yNyC(FxM) 4ClC.'N,c(FrTm) 2 s4 :fD4CH C1C2YNY Jcc lj___)' N 8C1 .C2 ..N.H2 .s(FrTM) 4C1 c2,N.s(F'TM) cross Hlc(rM) 2C1 .YH,,s(FrM) Figur 1: Qnitaize 1(H2'C2'N)-exriPYn Tuoexpmnts, dx ire arl cossocpenrtmam Hlys(Frm) ndaeIn the [f In ee expennPmphae p4 is set to x andpon derqing dui te b& transfiris appidfor heperiodlabie eiodlad cmross.A wterflohx pulse is appliedaftr thecrossexcperin phase (p4is y and prm are detledafor the eefzrstINEPT-step.Experntalparamten: A is "u to 1/(2*'Jca) andsetto3.2r; T=1/(2*1Jo) is38m; zm is the 2.5Gonl; G3=lrn, 40Gon'. c=l/'Jcc-M Graes: Gl=lns, -20Gonl; G2=5001s, ffcsNl/ 9 datwpel 2'HfC2',N119 aa pa r=1 -mGad . ie epeni (p4 =4 y,4 (-y) in & cross Phse cding V=x,2(-x),x,(-x),2x,2(-x),2x,(-x),x,2(-x),x.In adktion 6 is zsn t in expennrt ps=32x,32(-x);p6=8x,8(-x); in de co dinrmionMagnetizadtion Tmnsfer. Magrizatin to aie quadraue detection a State- TPPI[23]rrnurmr ihin diepulse ('rf) and crss ('mrs) expewrnt at de iicated tim pos and operatonsin the mfe traferthmy ( =x,(-x); (02=16x,16(-x); 3=2x,2(-x); -4=4x,4(-x) in the seqncz 68 Chapter2: F(HCN)-Experiment Scalar interactions between C2 , and both C1. and C3 , are suppressed by setting the total period in Extraction of which C2, is transversal to 25ms (+c=1/'Jc). \MCJLLJ~~~~~~~a quantitative F(HCN-experiment is similar to the r-,FDC2SA H2C2,NI9 (Eq. (7)). In case of the quantitative F(H2'C2',N)-experiment no optimization regarding TROSY enhancement or MQ was carried out. Since in agreement with the the observed cross-correlation rates were higher than for the parameterization for r DDCSA H2C2',Nl/9 parame~~~~~a F(HC)-experiment, no further optimization seemed necessary. 2.3.2.2 Resolving Xangle ambiguities with H2C2N19 DDCA F~~~~~~~~1"D Figure 18 shows that in the case of C,2-edo ribose puckering independent offers a second, H2'C2',NI 9 parameter, which potentially allows the removal of the ambiguity in X angle determination resulting from the interpretation of rFD',csII 9 alone. In this case, the actualvalue for X can be unambiguously determined by virtue of the best angular agreement between the two 9 , and rF'C s1A1 parameters. In contrast, for Cy3-edosugar puckering, rFlc`s but s"H2dC2',NI/9 sign are of opposite 9 sign but show a similar F(X) dependence. t3-enao 4- 4 '-pDDCSA C1'H1',N9 3 I 2 7 .72 MIq o-2 I -,- .... ~~~~~~~~C2H2N .'-'' ''-" -2 -2 r - D D' C S A '~C2'H2'N9 -3 0 90 180 270 0 360 180 x x[Ol Figur 18: angledepXnia in a (lid) rilse ecfmti 90 270 [0 I/ 9 (ds hlD)t for C2'eN (eif)and Cen9 rT nded aresiiLr Theparamnzationcuwfr theceher NllCS 9 (s i s) ad 69 360 Chapter 2: rF(HC-Experiment r DD,CSA Residue 19 Residue F,~~ H2'.m/9 [Hz] -2.3 -1.64 ____7_ Cs C2: 212 +2 268 +2 Z7 [0 ] 223 237 + 1 221 +2 259 2 202.6 ZC'HI 'N 302+1 e71C te (H2'C2N)-expn fre sbmisU7andC8 he 14-ntRNA.%cvnHi:T. uJCI 9 d, emrshae w n cxnrfimne aeraw derr CCsAI9 -deiudX at*&;Zx, nivem , a*. 7The Table 8:Resdts Xanl; %JW ZC2H2'N [0] 246 + 1 290 + 1 r in Ff 0.1Hz asd mirdfitnF andrC6/8H6/8 'N9 1, ,Nl/ Table 8 shows the results of the F(H2'C2',N)-experiment for residues U7 and C8 of the 14-nt RNA, which are in C2-endo conformation, together with the resulting X angles and the reference angles. Both F-rates alone result in two possibilities for . For these two residues, the parameterization and the experimental values for both cNI N1I/9 rDI' 9 FH2'C2, and rD,'%' IC',N19aesoni 1 1 9 are shown in Figure 19. The best agreement between r' ooAcISA - and rF'JD AsI 9 H2'C2',NI/9 -derived angles for U7 of 22 is Figure19. 'e bes agrement etwee CI,NI/9 THI " not in the region, where the reference angle is found. In this region, the agreement of the two experiments is 'only' 34° . Whereas rFHDo,fcs "H'C',NII9 results in a X value lower than the reference angle, is larger for rHD2DC',N9sA . X In contrast, for residue C8, the best accord of the two experiments (16 ° ) is found closest to the reference angle. Judging from the error of the experiment of about 2° , this difference is significantly smaller than the second best agreement (22°). It has to be noted that for this residue both cross-correlated relaxation rates point to a considerably larger X angle than found in the reference structure. = 4 4 3 3 2 C8 4-: - N- 2 rI 1 'r N- 1 -0 rDC8A 5( 8- ^ CWHl:Nl gi ° 11' -1 ------ : "V' I J 4- -t 3 -; - / 11 0 * - - 'S \ r-'°°'GSA rC2'H2'N1 -3 -3- 0 90 180 270 x[o] Figurw 19 Fr csAi(sd iu) ixd Itre&abe 'rf. Te *em 0 90 180 270 360 % [0] andr Pcssie zk x1 'wifor dx nmrd isMaid '. 360 rDDCSA C2'H2',Nl : 06V__97'e I -A rDDC&A C'lNl inXam 2CN DA (das hed )fr wh am sun by I&& dws. bet'wnd t crs-canan i z a* Wmuba t& im oys-"dawd ?daa 70 qthe14-ntRNA. U7( )adrig) exars rateag a shz by dd&ed ratesaregimv Chapter 2: F(HCN)-Experiment 2.4 CONCLUSIONS In this part of my thesis, I have introduced two new NMR-experiments aiming at the determination of the glycosidic bond angle X in oligonucleotides from the angular dependence of CG H-dipolar, N CSA cross-correlatedrelaxationrates (r'jc4 1 and rD4f s -,,csl/9 ' HICI,NI/ , -", a2nd2, 619 Nl,9) A /8 This comprised the development of a new pulse sequence as well as the critical examination of the data obtained from the experiments. 2.4.1 Pulse Sequence Development The pulse sequences developed here for the determination of DLoCSA, all rely on a quantitative approach. This method is advantageous to a J-coupled one in that the latter requires the evolution of coupling, which increases the number of signals in the spectrum and reduces the sensitivity both by a factor of 2. In general, however, the quantitative method requires a more elaborate pulse sequence in order to suppress unwanted relaxationpathways and transfer the cross and the reference operator as similarly as possible. In addition, while for the J-coupled approach either only one spectrum is necessary or both required spectra are obtained at the same time, the spectra in the quantitative approach are run in general consecutively due to the inherent different intensity of cross and reference signals, thus requiring higher stability of the experimental setup. Here, a quantitative approach was chosen, since the aim was to develop a method for the application to larger RNA molecules, where resolution as well as sensitivity become the limiting factors. During the course of my work on this project, an alternative method for the determination of dipole-dipole, CSA cross correlation in an HCN spinsystem was presented [27], relying on a J-coupled approach, which was applied to a 37-nt RNA. This work, however, focused on the analysis of the different factors contributing to dipole-dipole, CSA cross-correlated relaxation in regard to anisotropic overall and internal motion and the contributions of D ,CSA rHC' cN rFI CSAand rDDcsA No attempt was made to use as a structural parameter for the determination of X. The quantitative (HCN) developed in this report has been optimized enhancement during the long periods, in which a significant sensitivity improvement 3C for the TROSY is transversal. While this optimization constitutes for the base moiety because of the large CSA of the aromatic carbons, it has been shown that for the ribose moiety HCN-correlations can benefit from the use of 71 Chapter2: F(HC)-Experiment CH multiple quantum coherence (MQ) more than from the TROSY enhancement connected to C single quantum coherence [14, 28]. In principle, the introduction of MQ constitutes only minor changes in the pulse sequence scheme and could prove advantageous especially for larger molecules with unfavorable relaxation behavior. Since sufficient sensitivity could be obtained in reasonable experimental times (about a day), no optimization in this direction has been carried out. 2.4.2 Experimental Quality As shown by the application to two RNA molecules of known structure, X can be determined from r4' sI HI1',N 9 alone as well as from the ratio of C' 1/9 and F-basewith a precision of about 10° . This accuracy is equal to the one of the X angles resulting from the analysis of 3J(C,) coupling constants, which is the standard method for the determination of this angle to date. The precision is similar for the 14-nt and the 30-nt RNA, demonstrating that the underlying parameterization is valid in regard to the neglect of anisotropic overall motion and the use of 13 C and 1 5N (CS-tensors from mononucleoside crystals in the solid state. The agreement between the measured and the reference angles, however, is considerably better in canonical stem-regions than in the loop regions. This is surprising, considering that the agreement of experimental and theoretical F-base values is in general worse in the canonical regions as compared to the loop regions. This discrepancy could be due to the dependence of H'C 4 dependence on the 1 1 9,? 13 C on the 15N CS-tensor alone, whereas F-base exhibits an additional CS-tensor. It follows that the agreement between the experimental and 15 N CS-tensor. theoretical F-basevalues might not represent a measure for the correctness of the separate values of the 1 5N and the 13 C The CS-tensors and their conformational dependence of both tensors can unfortunately not be further analyzed based on this data. It is possible that while the reference 15N CS-tensors are applicable to oligonucleotides in solution, the The comparable quality of the fit to the reference values of z ' FHDI s 13C CS-tensors are not. angles determined from / 9 alone as compared to those derived from the F-rato, however, contradicts this assumption. To date, only one complete study of (mononucleoside 13C and 15N CS-tensors in model compounds crystals) is available [8]. All of these model compounds are in the anti conformation. With regards to a possible dependence of the CS-tensor on conformation, F(x) parameterizations will clearly benefit from a direct, residue specific determination of the nitrogen and 72 Chapter2: F(HC()-Experiment carbon (CS-tensor in the bases of oligonucleotides in solution. In principle, the fully anisotropic "5N CS-tensor can be determined from the geometric information conveyed in multiple cross-correlated relaxation rates correlating the N CS-tensor to the different neighboring dipole-dipole vectors or from the anisotropic chemical shift information extracted from samples in different alignment media. For proteins, a number of studies have been carried out along these lines aiming at the determination of the amide ' 5N CS-tensor in solution [29-31]. Although these methods assume a number of simplifications such as the axial symmetry of the CS-tensor or a common tensor value for all sites, they could be expanded to the site specific determination of the fully anisotropic CS-tensor of N9 and N1 in oligonucleotides. Since both angle determination methods from the F(HCN)-experiment can claim the same accuracy, the decision as to which of the methods is applied depends only on the time considerations and whether or not the system under investigationis dynamicallycharacterizedby NMR. Apart from knowledge about the 15 N CS-tensor, the angular interpretation of F1 1 DCSA -rates relies on information about the global and local dynamics of each molecule under investigation. Here, the accuracy of the method has been investigated by employing almost entirely rigid model molecules (only one loop residue is mobile for both molecules). In the case of conformational averaging, however, X cannot be extracted from the F(HCN)-experiment without detailed dynamic information. This requires the separate measurement of autocorrelated relaxation rates and a model free analysis of this data. Although this dynamic characterization is part of every extended investigation, in cases where this information is not available, the ratio of r? 4,, 9 molecular and F-basecan be used for angle determination. Although this method is more time consuming, it offers the same precision than rDcs a9 alone, whereas the parameterization requires no adaptation to either overall correlation time or magnetic field strength. However, it has to be noted that while formation of the F-ratioeliminates the dependence on concerted motions of the entire nucleotide, the effect of different motions in the base as compared to the ribose moiety, like e. g. rotations around X or ribose repuckering, is not removed and will impair angle determination even from the F-ratio. In addition, it has to be kept in mind that the same concerted motion can affect the two GH dipole-dipolevectors in different ways, leading again to a difference in the two F-rates. In case of a more complicated dynamic behavior the F(HCN)-experiment can be complemented by 3J(C,H) coupling constants. 73 Chapter 2: F(HCN)-Experiment The angles obtained from the g(HCN-experiment applied to the ribose moiety have been incorporated directly into the structure calculation of the 30-nt RNA in addition to a set of easily obtainable nOe distances. Inclusion of the additional restraints resulted in a significant improvement in the RMSD of the resulting structures, signifying that the direct %angle restraint can replace a more time consuming nOe analysis. The direct incorporation of the angle restraint is, however, only preliminary. In the future, the measured F-rate needs to be incorporated together with the F(X) parametenrizations. The F(H'C2'N)-experiment was intended to complement the F(HCN)-experiment and remove its inherent ambiguity in angle determination. Derivation of the F(X) parameterization showed that only in the case of non-canonical C2-endobut not for canonical Cy-ezdo sugar-puckering I",c2sAN/ 9 offers an independent parameter for the determination of X. Investigation of the F(H2'C2Nexperiment applied to the two residues in the 14-nt RNA, which adopt C2,-endoconformation did not result a significant improvement in angle determination. In addition, X angle determination from the experiment is dependent on a detailed characterization of the ribose pucker mode. A separate parameterization is required for each ribose pucker. Therefore, instead of using the F(H2'C2'N)experiment, ambiguous structural information from the F-(HCN-experiment can be complemented by nOe or scalar coupling constant information. Since the overall RMSD in case of the more anisotropic 30-nt RNA is of the same order of magnitude as the RMSD of the 14-nt RNA, we conclude that the effect of diffusion anisotropy is not significant and can be safely neglected in the size range of up to at least 30 nucleotides. Due to the linear dependence of cross-correlated relaxation rates on both the magnetic field strength and the overall correlation time t, the F(HCN)-experiment represents an interesting method for application to larger systems. 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Two- and three-dimensional HCN experiments for correlating base and sugar resonances in 15N,13Clabeled RNA oligonucleotides.J Bind NMR, 3, 721-727. 75 Chapter 2: F(HCN)-Experiment 16. Farmer, B. T., 2nd; Muller, L.; Nikonowicz, E. P.; Pardi, A. (1994). Unambiguous throughbond sugar-to-base correlations for purines in 3 C, 5N-labeled nucleic acids: the HsCsNb,HsCs(N)bCb, and HbNbCb experiments.JBi NMR, 4, 129-133. 17. Marino, J. P.; Diener, J. L.; Moore, P. B.; Griesinger, C. (1997). Multiple- Quantum Coherence Dramatically Enhances the Sensitivity of CH and CH2 Correlations in Uniformly 13C labeled RNA. JAm U(nSc, 119,7361-7366. 18. Sklenar, V.; Dieckmann, T.; Butcher, S. E.; Feigon, J. (1998). Optimization of tripleresonance HCN experiments for application to larger RNA oligonucleotides. J Magn Resan, 130, 119-124. 19. Brutscher, B. and Simorre, J. P. (2001). Transverse relaxation optimized HCN experiment for nucleic acids: combining the advantages of TROSY and MQ spin evolution. J Biond NMR, 21, 367-372. 20. Felli, I. C; Richter, C; Griesinger, C; Schwalbe, H (1999). Determination of RNA Sugar Pucker Mode from Cross-Correlated Relaxation in Solution NMR Spectroscopy. JAm (Cnem Soc, 121, 1956-1957. 21. Emsley, L. and Bodenhausen, G. (1992). Optimization of shaped selective pulses for NMR using a quatemrniondescription of their overall propagators. J. Magn Reon, 97, 135-148. 22. Geen, H and Freeman, R (1991). Band-Selective Radiofrequency Pulses. Janml of Matic Rsonane, 93, 93-141. 23. Marion, D.; Ikura, M.; Tschudin, R.; Bax, A. (1989). Rapid recording of 2D NMR-spectra without phase cycling - application to the study of hydrogen-exchange in proteins. J Magn Reson, 85, 393-399. 24. Shaka, A. J.; Barker, P. B.; Freeman, R. (1985). Computer-Optimized Decoupling Scheme for Wideband Applications and Low-Level Operation. Jaml qfMagncResonane, 64, 547-552. 25. Riek, R. (2001). Characterization of hydrogen bond lengths in Watson-Crick base pairs by cross-correlated relaxation. JMagnReson, 149, 149-153. 26. Dajaegere, A. P. and Case, D. A. (1998). Density Functional Study of Ribose and Deoxyribose Chemical Shifts. Jamml fPsica1 ChmistryA, 102, 5280-5289. 27. Ravindranathan, S.; Kim, C H; Bodenhausen, G. (2003). Cross correlations between "3 C'H dipolar interactions and 15N chemical shift anisotropy in nucleic acids. J Bior NMR, 27, 365-375. 28. Grzesiek, S. and Bax, A. (1995). Spin-locked multiple quantum coherence for signal enhancement in heteronuclear multidimensional NMR experiments. J Biorrd NMR, 6, 335339. 29. Tjandra, N.; Szabo, A.; Bax, A. (1996). Protein Backbone Dynamics and 1 5N Chemical Shift Anisotropy from Quantitative Measurement of Relaxation Interference Effects. J A m Cben Soc, 118, 6986-6991. 30. Fushman, D. and Cowburn, D. (1998). Model-Independnet Analysis of 15N Chemical Shift Anisotropy from NMR Relaxation Data. Ubiquitin as a Test Example. J A m Cern Soc, 120, 7109-7110. 76 Chapter 2: F(HCN)-Experiment 31. Boyd, J. and Redfield, C. (1999). Characterization of 1 5N Chemical Shift Anisotropy from Orientation-Dependent Changes to 5N Chemical Shifts in Dilute Bicelle Solutions. J Am CemSoc, 121, 7441-7442. 77 Chapter 2: F(HCN)-Experiment 78 Chapter 3: RNA Tetraloop Dynamics CHAPTER 3 Dynamic Investigation of RNA tetraloops by NMR 79 Chapter 3: RNA Tetraloop Dynamics Specific Aims The aim of this project was to contribute to the understanding of oligonucleotide stability and dynamics on a molecular level utilizing NMR spectroscopy. Autocorrelated relaxation measurements were used to report on the dynamic behavior of multiple carbon sites within every residue of two members of the same tetraloop family, the exceptionally stable cUUCGg tetraloop and the less stable uCACGg loop [1, 2]. The NMR relaxation data were translated into motional parameters by application of a model-free analysis and appropriate motional models, thus providing a highly resolved dynamic picture of both loop motifs in their ground state as well as at the initiation of melting of the uCACGg loop. TABLE OF CONTENTS 3.1 INTRODUCTION .................................................................................................. 3.1.2 82 The tetraloop RNA secondary structure motif ...................................................................... 82 3.1.2.1 The YNMG motif ............................................................................................................. 82 3.1.2.2 The uCACGg motif .......................................................................................................... 84 3.1.3 Dynamic investigations on RNA byNMR ............................................................................ 85 3.1.4 Autocorrelated relaxation rates ................................................................................................ 87 3.1.5 Model-free formalism ................................................................................................................ 89 3.1.6 Motional models ......................................................................................................................... 92 3.1.6.1 Wobble-in-a-cone Model (WIA )Q .................................................................................. 92 3.1.6.2 Gaussian Fluctuation Model (GAF)...............................................................................93 3.2 MATERIALS AND METHODS............................................................................. 3.2.2 94 NMR spectroscopy .................................................................................................................... 94 1 3.2.2.1 H, 5N-HSQC spectra ....................................................................................................... 13 3.2.2.2 C relaxation parameters ................................................................................................. 3 3.2.2.3 J(H,.,H 2) coupling constants .......................................................................................... 3.2.3 Relaxation data analysis ............................................................................................................. 94 94 95 96 3.2.3.1 Extraction of the relaxation data .................................................................................... 96 3.2.3.2 Model-free 3.2.3.3 3.2.3.4 Diffusion model ................................................................................................................ 97 Rotational correlation time .......................................................................................... 98 analysis ........................................................................................................... 96 3.3 RES ........................................................................................... ULTS 99 3.3.2 Temperature dependence of the imino proton resonances . 13 ................................................ 99 3.3.3 C relaxation analysis ............................................................................................................. 13 3.3.3.1 C relaxation parameters .............................................................................................. 3.3.3.2 Model-free analysis ........................................................................................................ 3.3.3.3 101 101 107 Dynamics of the 14-ntRNA ........................................................................................ 115 80 --- Chapter 3: RNA Tetraloop Dynamics 3.3.3.4 3.3.3.5 3.4 Dynamics of the 30-nt RNA ............................................................................. 119 M otional implications....................................................................................................123 DISCUSSION ......................................................................................................... 131 3.4.2 M odel-free analysis.................................................................................................................. 131 3.4.3 Dynamics of the YNM G tetraloop motif ...........................................................................134 3.4.3.1 Ground state dynamics ................................................................................................. 135 3.4.3.2 Melting of the uCA CGg motif.....................................................................................136 3.4.3.3 Biological implications................................................................................................... 138 3.5 OUTLOOK ............................................................................................................. 139 3.6 REFERENCES ....................................................................................................... 140 81 Chapter 3: RNA Tetraloop Dynamics 3.1 INTRODUCTION 3.1.2 The tetraloop RNA secondary structure motif Loops are stretches of 3 to 8 nucleotides connecting an intramolecular base paired region, thus allowing for a reversal of the strand direction, which is necessary for double strand formation. They are part of all larger structured RNA molecules. Tetraloops are the most common loop structures in ribosomal and messenger RNA [2]. They constitute key sites for folding nucleation [3, 4], tertiary structure formation [5, 6] and interactions with proteins [7-9]. These functions seem to require a well-defined structure, resulting in an in uw preference for sequences, which adopt thermodynamically stable secondary structures. The most common tetraloop sequence motifs are GNRA, UNCG and CUUG (N=any nucleotide; R=purine; Y=pyrimidine), which constitute over 70% of the tetraloop structures found n iw [10]. The members of these families each share a common fold. In contrast to the less stable GNRA family, UNCG tetraloops have not been found involved in tertiary structure formation and also do only rarely take part in RNA-protein interactions [11, 12]. 3.1.2.1 The YNMG motif Recently, the UNCG motif has been absorbed into the more general YNMG (M=A or C) tetraloop family [12]. The UNCG subfamily has been consistently structurally characterized both by NMR-spectroscopy [13, 14] and X-ray crystallography[15-17]. The structural features of the UNCG motif are shown schematically as well as within the structure of a cUUCGg-loop in Figure 1 and can be summarized as follows: Residues L1 and L4 form a base pair with L4 in the sn conformation. The base pair is stabilized by a bifrucated hydrogen bond (interactions a and b in Figure 1) and a hydrogen bond between the 2'-hydroxyl group of L1 and the L4(0 6 ) (c). The actual loop is formed by L2 and L3, which both exhibit C,-edo ribose puckering, thus extending the backbone by about 2A [18] and bridging the two sides of the stern. The base of L3 forms a hydrogen bond with the backbone phosphate group of L2 (d). The conformation of this residue is further stabilized by an intraresidual base-to-ribose hydrogen bond (e) and stacking interactions with the base of L1 (grey circles in Figure 1A). 82 Chapter 3: RNA Tetraloop Dynamics B 19 .4 S 5' 3' 5' 3' cUUCGgl [15] (B). Figul 1: Samc sedary s e of the UNCG tetra. nuif (4 and siu ef ad lis (ader Odnn bnzk) and grey boz), Stabiizg ieractan are gen as dashd lims (WatsoaCrideban dades (ase sta&ir. 4onm b The lo Ribose rtis in the C2'-endo nmt are soi in gre the grey stred base is in a syn residesare lab"d L1 to L4; the es f the doing bse pair am la iweaaios acrgiig to thestu awf S and S2. The Hbdgm thetetralosare (a) L4(N)-L 1(O); (b) L4(N)-L1(Q); (c) L1(02 )- L4(4; (4 L3(N4)-L2(PR); (e)L3(C)-L3(0);(~ L2(~-).L4(0. While residue L2 is stabilized by a hydrogen bond between its 2'-hydroxyl group and the base of L4 () in a UUCG-loop X-ray structure [15], no such interaction was found in the NMR [14] and both base and ribose moiety of L2 are free from any interaction with the other residues in the loop. In the X-ray structure, base stacking interactions are found between L2 and L1 and from L1 across the strand onto the closing base pair. From the NMR-structure as well as from a closer inspection of the X-ray structure, intrastrand stacking of L1 onto the closing base pair, as shown in Figure 1A, seems more likely. Structural investigations at low detail indicate that other members of the YNMG family exhibit structural characteristics similar to the ones of the UNCG motif [12]. In one particular case, the uCACGg motif, a detailed NMR structure [1] demonstrates a virtuallyidentical structure to the cUUCGg loop (Figure 2). In defiance of the structural similarities between the cUUCGg and the uCACGg, the thermodynamic stability of the latter is significantly lower [1]. While the cUUCGg loop is the most stable know tetraloop motif (TM=72 .9°C) [12, 13], the uCACGg loop melts already at around 45°C [1]. 83 Chapter 3: RNA Tetraloop Dynamics L2 Il itionq tdx cUUC-g[15] (dk gy) andd uCA d Mg nz4[1] (izgt gy). Figut 2 S : pn The decreased stability of the uCACGg loop has been attributed to its U:G wobble closing base pair, which supposedly has a destabilizing effect in contrast to the GG base pair of the cUUCG loop. The general relevance of the closing base pair for loop stability is supported by studies showing that tetraloop stability is decreased upon reversal of the CG closing base pair to a G:C base pair [19]. This has been explained by the different propensity of interstrand base stacking interactions between the first loop residue and the closing base pair. 3.1.2.2 The uGACGg motif The 30-nt uCACGg hairpin RNA studied in here constitutes a part of the regulatory cloverleaf structure in the 5'-non-translated region of the coxsackievirus 3B (CVB3) genomic RNA (Figure 3). The loop is part of the stem-loop D (SLD), which constitutes the major recognition site for the viral protein 3CDP ° [1, 20, 21], the precursor of the protease 3 ' 0.° and the polymerase 3Dp Interaction of 3CDP ° with SLD is an essential step in the assembly of the viral replication process [22, 23]. In utro interaction studies have shown that SLD alone is sufficient for binding of 3CDPr° . Replacement of the uCACGg by other members of the YNMG family (cUGCGg) does not impair the interaction with 3CDP ° [1, 24], indicating a structure based rather than a sequence based recognition mechanism. 84 Chapter 3: RNA Tetraloop Dynamics A i t- Translation Start I 5' -NTR Coding Region B SLD SLA 5' Figure 3:A' Shmuc (NTR) is iicat uralprn 3' "pesenan f theacsadk iem B3 the 5'-dowdafisbhigbigba B: C i 0? hesxnay smuae dafsewSary smcw and nn f the5'-non-trarlsad rgm aw The bidng site f the 3CD- is viSa!t 3.1.3 Dynamic investigations on RNA by NMR Autocorrelated relaxation parameters constitute a measure of the rate of decay of non-equilibrium magnetization through different mechanisms. Since NMR-active nuclei can be viewed as tiny magnets, their motion will result in magnetic field fluctuations, which cause nearby nuclei to relax. The rate of relaxation therefore constitutes a measure for a nucleus dynamics. The contribution by other spins to the relaxation behavior of a nucleus depends on the internuclear distance as well as their magnetic susceptibility. Therefore, e. g. a protein backbone amide nitrogen experiences primarily the relaxation effect due to the proton directly attached to it. Hence, the analysis of the 15N relaxation data will report on the dynamics of the amide N-H vector. The quantitative dynamic analysis of NMR relaxation data is most simply and therefore most widely applied to systems, which can be treated as isolated I-S spin systems. In this, I represents a hydrogen spin and S is the 85 Chapter 3: RNA Tetraloop Dynamics heteronucleus ( 3 C 15, whose dynamics is studied. It is assumed that the heteronucleus relaxes predominantly due to the I-S dipolar interaction and its own CSA. In proteins, the amide nitrogen in 15N only labeled molecules represents a residue specific dynamic probe (all amino acids can be sampled except proline, which does not possess an amide proton) exhibiting to first approximation the relaxation behavior of an isolated I-S spin system (Figure 4, left). In contrast, in oligonucleotides, due to the faster imino as compared to amide hydrogen exchange, NH moieties are only present in base paired regions and in most cases, only one of the bases in a base-pair can be sampled (Figure 4, right). Protein I --..A ,..o-- RNA P-1 N WI I 1./V k - I&- -A. Figure 4:NH-tars asdyancpri inprmei (10 and rmeicaids (nigbt. In order to obtain more detailed dynamic information on RNA, 15N relaxation measurements have to be complemented by the investigationof other nuclei. 13C relaxationcan report on both the ribose and the base moieties of all nucleotides. It has, however, to be noted that unless selective labeling schemes are employed, C in the bases of guanosine and adenosine and C2 in adenosine represent the only isolated CH groups in nucleic acids. For the remaining S spin system relaxation but the effect of neighboring 3C 13C sites, 13C relaxation does not follow I- nuclei (CCdipolar contribution) has to be taken into account in a quantitative analysis. In addition, the chemical shift (CS) tensor of both the aromatic and the aliphatic carbons is not axially symmetric [25, 26], which further complicates the analysis. Because of the afore-mentioned complications, oligonucleotide C relaxation data has been obtained and analyzed by resorting to selective labeling techniques in order to create isolated I-S spin systems, like selective labeling of specific "3Csites [27-31], uniform partial 86 13C enrichment [32, 33] or Chapter 3: RNA Tetraloop Dynamics measurement at 13C natural abundance [34-36]. If data was obtained on uniformly labeled samples, the analysis was either restricted to the isolated C2 and C8 spins in adenosine and guanosine [37], small systems, in which the CCdipolar contribution is small compared to the CH contribution [38, 39], the data was only qualitatively analyzed [40-42] or a larger number of relaxation parameters has been acquired [42]. In order to investigate the molecular basis for the higher stabilityof the cUUCGg compared to the uCACGg motif, the 14-nt hairpin RNA comprising a cUUCGg tetraloop and the 30-nt SLD, containing the uCACGg motif have been studied by relaxation measurements at 298K, where both loops are stable and at 317K, where the uCACGg loop has started to melt, while the structure of the cUUCGg loop is unperturbed. At both temperatures R,, Rp and hetnOe measurements have been carried out for C1 and CQin pyrimidines and C1 . and C8 in purines (Figure 5). In order to obtain quantitative dynamic information, the relaxation data was subjected to a model-free analysis and translated into motional models. In addition, the ' 5 N line-width was studied at both temperatures. A NH2 I I N H OH Figure 5: Imesgtd 1 Cs (liZitgey)inps (4) andpyqiid OH (B). 3.1.4 Autocorrelated relaxation rates Relaxation of a spin S in an I-S spin-system is dominated by the I-S dipolar interaction and the S chemical shift anisotropy (CSA). In case of a 13 C spin with an attached proton, the spin-lattice (R1 ), the spin-spin (R) and the steady state nOe (hetnOe) relaxation parameters are described by the following (Eq. (1)-(3)) [43]: 87 Chapter 3: RNA Tetraloop Dynamics R 1 =d (1) 4 [J(oH - CO) + 3J(coc ) + 6J(COH+ OC)]+ C2 J(cOC ) R2 =d8 [4J(O)+J(H - c)+3 J(coc)+6J(co H ) +6J(CO H +CO)] (2) 2 + HetnOe=l+(d 2 /4R, (3) In this, 6 [4J(O) + 3 J(coC )]+ Rex 0 H /c X6J(cH +C )-J(H % -C )] and c0 c are the Lamor frequencies of H and 1 3 C, respectively, J(co) is the spectral density function at frequency a, Rex is the parameter accounting for the conformational exchange contributions; d = uohycyH /(8 rCHr 2 ) and c = COCAcc //[ describe the dipolar and the CSA interaction, respectively, uo is the permeability of the vacuum; h is Planck's constant; is the gyromagnetic ratio of nucleus i; r, is the internuclear distance between C and H; Ac c is the carbon CSA The principle dependence of the relaxation parameters on the overall rotational correlation time tc is shown in Figure 6. While R1 exhibits a maximum, R2 increases continuously with c. This difference arises from the dependence of R2 (Eq. (2)) but not of R, (Eq. (1)) on a J(O) term, which is negligible at lower tc values but becomes more and more relaxation relevant with increasing tc. For macromolecules such as proteins or RNA, Tcusually lies right of the R, maximum and consequently small R1 but large R2values can be expected. 88 Chapter 3: RNA Tetraloop Dynamics .-- 100 C I ;... .; :-.: .,. C.;., . , :.-- - .:-''.:.':'.:'':'' U)~~~~~~~ 7' ~~'10 -in 0~~~~~h',"¥""'- ___ __ ':"'"'""' it! .'.'"'.', v'ai .-- :..:-.Pne rO w 0 I . , 2 . I 4 . 6 I 8 w I 10 'r [ns] Figuwe 6:Depen H torl fR 1, R 2 and thehet on r . A rmngeticfield smh lf1.09A hs been assund Thercngi f themIas qf 600MHz, a CSA of 60ppmanda C stuiedn e has ir at bygreysd 3.1.5 Model-free formalism The model-free approach [44, 45] has been developed in order to translate autocorrelated relaxation rates into general dynamic parameters, which are free of any underlying motional model, hence 'model-free'. This is desirable, since NMR relaxation data unfortunately does not contain any information on the nature of the motions causing the relaxation. The model-free formalism is the most widely applied method for the dynamic interpretation of relaxation data. Spin relaxation is considered simplified within an isolated I-S spin system, e.g. the relaxation mechanisms are restricted to the I-S dipolar and the S CSA relaxation. Its output are the so-called model-free parameters. Different models of varying complexity have been developed to describe the amplitudes and time scales of motion (Figure 7): In the simplest case, these consist of the generalized order parameter S2 , which is a measure for the spatial restriction of the internal motion, and the effective correlation time Tedefining the time scale of motion (Figure 7). Assuming isotropic diffusion, the spectral density function can then be expressed as follows (Eq. (4)): (4) J(co) = 2 S22 +( _ o892 89 )r Chapter 3: RNA Tetraloop Dynamics In this, c is the overall rotational correlation time of the molecule and 1/c=l/'Cc+l/c e. If 'Ct is small (tc < lOps),the dynamics can be described exclusively by S2 (Model 1, Figure 7A). In the presence of slow motional events in the milli- and microsecond range Models 1 and 2 can be extended by a chemical exchange or line-broadening term Rex (Figure 7C&D, Model 3& 4). In principle, the Re-term accounts for the sensitivity to R2 for slow time scale motions. In the modelfree analysis, R= is directly added (see Eq. (2)). Direct interpretation of R= is however difficult since the requirement for this term can arise not only from its own conformational exchange but also other sources like chemical exchange of adjacent parts of the molecule. In cases, in which two fast motions with time scales differing by at least one order of magnitude take place, an extended model-free formalism has been developed [46] with a separate S2 for each motion, S 2 and S2 (Figure 7E, Model 5). (5) J(o)=2 (1-S 2 )rf S 2rc L+crL 1+2 C + o 2T 2 ~f (S-S2)T + co2 J In this two time-scale model (Eq. (5)), it is assumed that the contribution of the faster of the two motions can be neglected (f+O0). Therefore, while the faster motion contributes to the overall S2 (S2=S 2 *S ), the term containing the fast effective correlation time f is left out. Similar to simpler models, the time scale of the slower internal motion ;s is included in will therefore not be discriminated from Cein (1/T =l/ Tc in the +l/t1) and the following. In the case of an anisotropic shape, the molecule does not longer tumble with one isotropic rotational correlation time (Figure 7F). For the case that D =D,7 =D1 , the spectral density function of a symmetric top rotator (D =D I ) or an axially symmetric top molecule is obtained (Eq. (6)): (6) Jq( ) I(jq, +jq,L J+q,mean ,in which the reduced spectral density functions is: (87) ~jq,m 2rm +9(0qm) 90 ------ Chapter 3: RNA Tetraloop Dynamics A C B R. o-22 s2 IN .. E D ' . . .-.. : F R-, Figur Z7: Midd-fiwrparant fr a GH spasstem thna n e thaturns icirad y th de oerall aal a vatir t c(A-E) or amsfally y (l. A Maidel 1;Fast er mo onetrn sale ( < lOps;S241). B: Modd 2; Skver ire mtian (r,> 0lps).C Mdd 3 Exend Modd 1 rwgi te dxnical exdmr xwa (rf< lOps;S2 41, R A2).D:Modd 4; Ext d M 0). E:Moadl 5; Thotnm scaleextended rndd 40, r ; 0) F A nisp axiallysynt zt M dion D Il and D ae the g and the short axis f te ax We2, oorping the S2 paranmt, In tbisa y syn S and S heoa nda nt/ibution(rc> 1Ops,RE • forslowandfastnii tul ling d/insm teor, arc7wd the short and the long axis of the rraule and rcm ean is the aeragd 91 enicalexdnge 2 is desti <; by nation rzI and r aye ti (S te at/ntis f s; Chapter 3: RNA Tetraloop Dynamics In Eq. (7), m={ Il, I , man}. The correlation times can be related to the diffusion tensor components Di1 and DL according to Eq. (8): II-,m = D i +n'(DI, -D I (8) with n=O for m= L, n=1 for m= j and n=2 for m=nran 3.1.6 Motional models Although the advantage of the model-free analysis is that a specific motional model is assumed a prio, in the end, a motional picture from the dynamic analysis is desirable. It has, however, to be kept in mind that the relaxation data do not report on the nature of the motion but only on its extent. Therefore, any motional model has to be examined critically, since it might origin more in our desire to condense the data into a picture than it reflects the actual processes in the molecule. Two slightly different models for the motional interpretation of S2 are presented in the following. 3.1.6.1 Wobble-in-a-cone Model (WIAC) NH2 H OH Figure 8: 'WaWu na-ame-nrddfor Cr-Hr arndC8-H8in ader The so-called 'Wobble-in-a-cone' (WIAC) model [47] allows modeling of the motions of the CH vector as motions on a cone of semiangle Oo.(Figure 8) with the time scale order parameter as follows (Eq. (9)): S 2 =[1/2cos0 0 (1+cos9 0 )]2 (9) 92 ~ ~~~~~~~ ~ ~ ~ ~ ~ ~ ~ ------ ce. 00 is related to the Chapter 3: RNA Tetraloop Dynamics 3.1.6.2 Gaussian Fluctuation Model (GAF) .0 X IH2 N 2 L. H OH OH Figur 9: GAF-nllfor Ct118amEd X in adep The GAF model [48] represents a restricted version of the Wobble-in-a-cone model since it describes a Gaussian distribution of bond vectors on the surface of a cone (Figure 9). The S2 parameter and the angle between the CH vector and the cone-axis is defined as (Eq. (10)): (10) S 2 =1 3 sin2 cos2 l - e- X ) -sin2 4 ( 1 -e 4 )l In this, fi is the angle between the C-H vector and N-Ca,, the director axis of the cone, and a 2 is the standard deviation of the fluctuation in the azimuthal angle, which corresponds to the fluctuation inmx. 93 Chapter 3: RNA Tetraloop Dynamics 3.2 MATERIALS AND METHODS 3.2.2 NMR spectroscopy The NMR samples of the 14-nt and the 30-nt RNA were prepared as described in the Material and Methods section of Chapter 2. In case of the 30-nt RNA, the relaxation data was obtained from two samples. One, with selective 3 C and ' 5N labeling in the guanine and cytidine residues was obtained as described as described in Chapter 2. The second exhibits selective labeling in the adenine and uridine residues and has been obtained with a similar synthesis as well as sample preparation scheme. All measurements 1H{13 C/15 N} were carried out on a 600MHz Bruker spectrometer equipped with a 5mm Z-Grad TXI probe at 298K and 317K. The spectra were processed using Bruker NMRSuite (XwinNMR 3.5) programs. 3.2.2.1 H,SN-HSQC spectra 'HK 5N-HSQC spectra were obtained with the nitrogen carrier set to 154ppm, the spectral width in the indirect dimension was 20ppm and 64 complex points were acquired in the indirect dimension with 4 transients per t increment. The proton carrier was at 4.7ppm with a spectral width of 25ppm and complex 1024 points were acquired. For the 14-nt RNA, in addition to measurements at 298K and 317K, a spectrum was obtained at 323K. 3.2.2.2 uC relaxationparameters R1, Rip and heteronuclear nOe data were obtained for C1 , C6 and C8 from 13C modifications (Appendix A3.1) of methods introduced for 1 5N autocorrelated relaxation measurements [49-52]. Separate experiments were conducted for C1, and the aromatic carbons with the carbon carrier frequency set to 89ppm and 139ppm, respectively. The spectral width was 6 ppm for Cr and 5 ppm for C6/C. 64 to 100 complex points were acquired in the indirect dimension depending on the available spectrometer time. The proton carrier was set to the water frequency (4.7ppm), the spectral width was 10ppm and 1024 complex points were acquired in this dimension. Off-resonant carbon Q3 pulses (512s) were applied during carbon evolution with an offset of -7500 Hz or-5000 Hz in order to suppress the J(C,C 2 ) and lJ(Cs,C) coupling, respectively. R1 and Rp data was obtained with 8 scans, the hetnOe with 16 scans for each t,-increment. The 2D-R- and Rlp-subspectra with 94 Chapter 3: RNA Tetraloop Dynamics varying relaxation delays were acquired in interleaved pseudo-3D experiments were also recorded experiments. The hetnOe interleaved, with alternating proton-presaturated and non- presaturated transients. The interleaved spectra were separated by a slightly modified Bruker standard macro (splitinvnoe, Appendix 3). For the acquisition of R1 relaxation rates, spectra with a varying relaxation delay TM of lOmns, 50mnis, 100ms, 200ms, 400ms, 700ms, s and 1.5s. Spectra with rM=50ms and 400ms were recorded twice. Rp rates were acquired as described in ref. [51] and [52]. Random length proton decoupling pulses were applied during the carbon spin-lock period (option d in ref. [511). Adiabatic Mulder pulses [52] were used to rotate carbon magnetization into the transversal plane. A spin-lock field of 3.6 kiHz was applied for the variable rM delay (M=12ms, 24ms, 36ms, 48ms, 64ms, 8ms, 104ms, 128ms). Duplicate measurements were carried out for 24ms and 80ms. The spin-lock offset was set to 2000Hz. Th e 2000HIz. The measured Rameas-rates contain a spin-lock offset and spin-lock power dependent contribution of R. From Ras (11) and Ri, R2can be extracted followingEq. (11): R2= R meas- R1 cos2Os 2 sin 2 Os In this, 9, is the angle of the effective spin-lock field for each nucleus with the B0 field. 9, is defined according to Eq. (12): (12) Os =tan-( s ,in which v is the spin-lock field strength in Hertz and .2s is the resonance offset from the spin- lock carrier in Hertz. 3.2.2.3 3 J(Hr,H .) 2 3 J(H .,H ,) 1 2 coupling constants were obtained from E.COSY splittings of H1 ,G2 and H 2,C, cross-peaks in a 2D- HCCH-E.COSY experiment [53]. The carbon carrier frequency was set to 77ppm with a spectral width of 40ppm and 128 complex points in the indirect dimension. 64 transients were acquired for each t increment. The proton carrier was positioned on the water resonance at 4.7ppm. 1024 95 Chapter 3: RNA Tetraloop Dynamics complex points were acquired with a spectral width of 10ppm. Errors were obtained from duplicate measurements. 3.2.3 Relaxation data analysis 3.2.3.1 Extraction of the relaxation data From the spectra, peak intensities were obtained using Felix2000 (msi) macros (autopkhpos.mac, Appendix 3.2). The hetnOe constitutes the ratio between the peak intensities in the spectrum in the presence and in the absence of proton presaturation. The error was obtained from duplicate measurements. In cases, where no duplicate measurement has been carried out, an error of 1% (0.01) has been assumed. For both R1 and R1 p, mono-exponentional 2-parameter decay curves were fit to the peak intensity versus relaxation delay correlations using the macros compkhuncledit2.s, myfx2gnu2p.s, myrun.r2.2ps and mycurvefit2table provided by Palmer and co-workers [54]. The error on the data incorporated into the fitting procedure can be calculated bythe macro compkhuncledit2.s from the different peak intensities obtained in the duplicate measurements of two time points. This errors, however, frequently proved to be too small for the subsequent fitting routine to produce relaxation rates within the a =0.05 critical value. Therefore, the error, which was defined differently for each time point by the program, was increased to the maximum calculated error for each time point. In some cases, even this error did not suffice. In this cases, the error was increased in small steps until all residues could be fit. It has to be pointed out, that this procedure did not have any effect on the resulting relaxation rates but did only change the resulting uncertainty in the values. 3.2.3.2 Model-free analysis The model-free analysis of the relaxation parameters has been carried out using the program Modelfree 4.15 by Arthur G. Palmer [55]. Modelfree is able to fit the relaxation data with the 5 different dynamical models (Figure 7). While initial runs were performed separately for CQ and C/C4, final Modelfree runs were carried out with the combined relaxation data. During model selection the number of models accessible for a given residue is defined by the number of relaxation parameters obtained for this residue, since the number of fitted parameters 96 Chapter 3: RNA Tetraloop Dynamics must not exceed the experimental parameters. Model selection followed the procedure recommended in ref. [55] and is briefly described in the following: Occams razor was applied in that the simplest model fulfilling the required level of certainty was selected, even if a more complicated model improved the fit. Accordingly, the selection process was started applying Model 1 to all residues. The goodness-of-fit between the model and the experimental data was determined by creating 200 randomly distributed synthetic data sets using extensive Monte Carlo numerical simulations. These data sets represent the random variations in the fitted data arising from the error of the experimental data. The results were used to determine the cumulative probability distribution and the a =0.1 critical value of the sum-squared error X2. Model 1 was selected, if the x 2 of the residues was below the a =0.1 critical value. For the remaining residues, model 1 was compared to either of the two-parameter models using an F-test analysis, which is included in Modelfree. If the 0.2 critical value of the F-test analysis was exceeded, the more complicated model was selected. If the data could not be fitted with either of the two-parameter models and the at=0.1 critical value for Model 1 was not significantly exceeded, the data was still fitted with Model 1. For the remaining residues, the three-parameter models (Model 4 and 5) were applied and compared to Model 1 accordingly. If the 0.2 critical value of the F-test anaylsis was exceeded, the respective model was selected, otherwise, the residues were considered not fittable. The x2 values are dependent on the varying error resulting from the preceeding curve fitting procedure for R, and Rip. In the model-free analysis, a general error of 5% has therefore been assumed for R1 and Rp. This error was considered appropriate to account for the possible error in the assumed CSA values together with deviations in the pdb-coordinate file from the actual structure. In case of the hetnOe, the error resulting from duplicate measurements sometimes amounted to considerably less than 1%. In order to fit the data in the model-free analysis, the error was elevated to 1%. A lower error was applied for the hetnOe than for R1 and R2 since its dependence on anisotropic diffusion is not as pronounced. 3.2.3.3 Diffusion model The diffusion model was selected by fitting the relaxation data to an axially symmetric or an isotropic diffusion tensor in the program Modelfree. In addition, the diffusion tensors has been determined from hydrodynamic calculations using the program hydroNMR [56] based on the pdbcoordinate files of the molecules. 97 Chapter 3: RNA Tetraloop Dynamics 3.2.3.4 Rotational correlationtime c The rotational correlation time c was determined by different methods. On the one hand, c was determined from the 13C relaxation data using the program Modelfree, where it constitutes a part of the diffusion model optimization. On the other hand, it was taken from the output of the program hydroNMR, which performs a hydrodynamic calculation based on a pdb-coordinate file. In addition, a rough estimate of c can be obtained from a simplification of Eq. (4). In the absence of internal motion (S2 -1 and -rz--), J(co) simplifies to Eq. (13): J(§) = rc +co2 r2 ,and Tccan be determined from the R2 (Eq. (2)) over R 1 (Eq. (1)) ratio according to Eq. (14): (14) J 2 R. 2 2 98 Chapter 3: RNA Tetraloop Dynamics 3.3 RESULTS 3.3.2 Temperature dependence of the imino proton resonances The exchangeable imino protons constitute detectors for the presence of hydrogen bonds in nucleic acids. If an imino proton is detectable, it is engaged in a hydrogen bond and the peak linewidth is an indicator for the strength of the interaction in respect to its structural as well as its dynamic features. If the imino proton is not part of a hydrogen bond, it exchanges with the solvent water and is therefore not detectable. Figure 10 shows the 1H, 15N-HSQC spectra of the 14-nt and the 30-nt RNA at 298K and 317K. In the following, relative resonance intensities have been used as measures for the line-width. Since the integral of a resonance is invariant, the intensity reflects the line-width in a comparative analysis. All imino resonances of the 14-nt cUUCGg RNA stem residues including the closing base pair are of similar intensity at room temperature. A U7 C8 U ............. oil ppm 6 144- CS--G: 317 G9 146- A4-Ull 3 _Gt0 148- C - G12 150- G2-C13 152- *G12 G2 154- G5' 3'-C14 5' 3' 156158160162- ul. . 14.0 . 13.5 . 13.0 1 2. 12.5 1 2. 12.0 1 .. 11.5 1 11.0 1.p0. . 10.5 1 .0 10.0 ppm B 0 5 el6 na _ C14-- Oj G1t' - PP" c" ....... UlJ- G1 8 144 uCG!, A tL - 'If' 0 U11t- A2 G l_ C 21 G0u8 C 2 223 15 U 2 4 154 U" GU25 154 G. C7 U s -C A 4 -U 2 7 C3- G28 G2_ U2 ' G 1 - C3 0 5' 4 15 3' 154 16( 16 13.5 13.0 12.5 12.0 11.5 11.0 10.5 10.0 ppm n Figuw 10: lHl 5 N-HSQCspmra jhe 14-nt(A and de 30-nt RNA (B) at 298K(to) and 317K (boari. ID sli:e grey). dmogh he resonanmnv of bt the basepar in ds an the tw a4amm basepans am gw (shaded nm 99 Chapter 3: RNA Tetraloop Dynamics The G9 imino resonance is only slightly smaller in intensity, signifying that the U6:G9s base pair is about as stable as the Watson-Crick base pairs in the sternm. At 317K, the G9 imino resonance is significantly decreased, indicating that the U6:G9s base pair is still present but considerably weakened. All the other base pairs, even the loop closing base pair, remain stable. The G9 iino resonance is still present at temperatures as high as 323K (data not shown). In case of the 30-nt uCACGg RNA, the iino resonance of the loop base pair C14:G17 is undetectable at 317K and the resonance of the closing base pair U13:G18 as well as the one of U19 adjacent to it are weakened. This relative decrease in signal intensity at similar positions in the hairpin demonstrates the higher stability of the cUUCGg as compared to the uCACGg loop. Observation of the imino resonances alone, however, does only report a limited number of residues, especially since three residues of both loops do not show an imino resonance in the spectrum. In addition, imino resonances undergo exchange reactions that complicate the analysis of their relaxation behavior. 100 . Chapter 3: RNA Tetraloop Dynamics 3.3.3 3Crelaxation analysis 3.3.3.1 3Crelaxation parameters R 1, R2 and hetnOe data of C1, and C6 or C of all residues in the 14-nt and the 30-nt RNA at 298K and 317K are sunmmarized in Table 1 to Table 4. Typical R 1 and R2 relaxation delay curves for the 14-nt RNA are shown in Figure 11. RI [s' ] G1 G2 C3 A4 C5 U6 U7 C8 G9 G10 Ull G12 C13 C14 C 6 /C 8 3.54+0.04 3.62+0.06 4.43+0.07 3.68+0.04 4.60+0.10 4.53+0.06 3.49+0.04 4.08+0.06 3.30+0.03 3.69+0.04 4.68+0.07 3.71+0.04 4.48+0.09 4.45+0.08 R2 [s4] C1 2.50+0.16 2.68+0.04 2.76+0.03 2.81+0.04 2.85+0.04 2.89+0.04 2.59+0.06 2.54+0.08 2.62+0.04 2.65+0.04 2.75+0.03 2.77+0.04 2.86+0.04 2.79+0.04 C 6 /C 8 9.42+0.57 9.30+0.97 13.39+1.22 10.35+0.63 13.05+1.80 13.25+1.16 12.65+0.66 14.22+1.20 11.75+0.50 10.01+0.55 14.02+1.24 8.75+0.69 13.77+1.59 13.23+1.45 C 6 /C 8 C1 9.32+0.57 1.12+0.03 1.12+0.03 10.24+0.71 8.42+0.47 1.10+0.01 8.48±+0.62 1.14+0.001 8.39+0.51 1.10+0.01 8.47+0.58 1.10+0.02 8.33+1.00 1.16+0.03 1.10+0.02 6.13+1.00 9.84+0.68 1.12+0.01 8.35+0.57 1.13+0.02 8.88+0.50 1.09+0.02 9.55+0.60 1.10+0.01 7.83+0.49 1.10+0.003 1.13+0.01 6.78_+0.45 Cq,. 1.21+0.00 1.14+0.02 1.16+0.02 1.18+0.002 1.15+0.02 1.14+0.002 1.12+0.09 1.11+0.05 1.15+0.003 1.12+0.05 1.15+0.01 1.13+0.03 1.18+0.03 1.22+0.04 t e 14.ntRNA at 298K svndaton rates Cf/C8 and Cvqb Table l:A u R2 [s 4 ] R1 [s"] G1 G2 C3 A4 C5 U6 U7 C8 G9 G10 Ull G12 C13 C14 HetnOe HetnOe c 6 /C 8 CT C6 /C 8 C, 3.78+0.09 3.92+0.09 4.69+0.12 4.11_+0.10 4.99+0.14 5.08+0.13 3.62+0.08 4.54+0.11 3.57+0.07 3.94+0.08 5.08+0.14 3.99+0.08 4.88+0.13 4.92_0.13 3.20+0.09 3.38 +0.03 3.51+0.04 3.53+0.04 3.57+0.04 3.51±0.04 3.23+0.05 3.32+0.07 3.30+0.04 3.34+0.04 3.52+0.04 3.46+0.03 3.53+0.04 3.23+0.03 7.03+1.49 11.51+3.14 9.52+2.29 7.37+1.72 9.09+2.68 9.26+2.37 9.31+0.94 9.93+1.59 8.99+0.97 7.45+1.54 9.71+2.41 10.30+2.86 9.58+2.36 9.33+2.01 7.73 +0.40 6.50+0.36 6.33+0.37 6.26+0.35 6.54+0.41 5.15+0.53 5.73+0.77 7.34+0.44 9.53+0.63 6.48+0.36 6.57+0.32 6.19+0.37 5.06+0.28 Table 2:Autama natan C6 /C8 1.22+0.01 1.18 0.002 1.13+0.002 1.16_+0.01 1.20+0.007 1.15+0.01 1.21+0.002 1.16+0.003 1.19+0.001 1.19+0.001 1.15+0.01 1.18+0.009 1.15+0.007 1.15+0.002 C1 1.23+0.02 1.18+0.01 1.17+0.01 1.21+0.00 1.21+0.01 1.18+0.01 1.23+0.02 1.22+0.02 1.21+0.01 1.24+0.30 1.21+0.02 1.21+0.03 1.19+0.02 1.32+0.01 ratesofQC/C8andC, fte 14-rtRNA at 317K 101 Chapter 3: RNA Tetraloop Dynamics G1 G2 C3 A4 C5 U6 C7 U8 G9 G10 Ull A12 U13 C14 A15 C16 G17 G18 U19 A20 C21 C22 HetnOe R2 [s ] RI [s] C1 , C1 C 6 /C 8 C 6 /C 8 1.70+0.03 1.64+0.03 1.91+0.04 1.58_+0.003 1.94+0.04 . . 2.04+0.03 2.02+0.002 1.59+0.02 1.59+0.02 2.06+0.004 1.63+0.001 2.00+0.002 1.98+0.03 1.49+0.001 1.90+0.03 1.53+0.09 1.65+0.02 2.00+0.003 1.64+0.003 1.89±0.04 1.99+0.04 C1 . 1.06+0.03 1.11+0.01 1.18_+0.01 1.07+0.02 1.12+0.02 c 6 /c 8 26.53+1.41 25.02+0.93 37.19+2.15 23.01+1.01 35.54+2.42 1.04_+0.02 1.10+0.02 1.01+0.02 1.15+0.02 1.11+0.02 1.13+0.02 1.15+0.03 1.27+0.02 1.38+0.05 1.30+0.02 1.40+0.01 1.25±0.02 1.22+0.02 1.06+0.02 1.20+0.01 1.12+0.01 36.36+2.03 32.04+0.43 24.74+0.97 24.89+0.90 32.27+0.75 24.22+0.40 28.72+0.33 36.58+1.99 16.37+0.13 33.71_±1.42 31.31+4.64 23.92+0.70 29.27+0.15 23.83+0.39 36.35+2.24 37.33+2.13 1.11+0.01 30.50+2.35 1.08+0.01 24.14+1.07 1.08+0.02 38.81+4.99 1.10+0.01 29.71+2.01 1.09+0.01 25.25+1.07 1.07+0.01 22.96+1.14 25.50+1.44 1.10+0.003 1.12+0.02 28.44+1.90 15.35+2.26 1.26+0.002 1.14+0.01 22.19+1.70 24.45_+1.18 1.06+0.01 1.13+0.01 25.50+1.30 1.06+0.004 1.12+0.004 24.03+1.28 25.20+1.60 1.09+0.003 1.07+0.01 27.43+1.84 1.96+0.002 1.96+0.001 1.55 +0.02 1.94+0.004 1.59+0.02 2.03+0.001 1.89+0.03 1.17+0.03 . 1.28 +0.04 31.52+0.30 30.90+0.09 26.46 +1.06 33.66+0.38 23.69+0.94 28.45+0.46 37.37+2.02 21.81+1.22 . - 28.92+1.59 27.21+1.56 25.40+1.41 - 1.16_+0.004 1.14+0.02 1.07+0.001 1.10_+0.01 1.09+0.004 1.17+0.01* 1.15±0.01* 1.11+0.01* 1.12_+0.01 1.08+0.01* 1.10+0.01* 1.08+0.001 1.12+0.01* 1.07+0.01* 1.11+0.003 1.17+0.01 1.15+0.03 1.12+0.01* 1.23+0.01 1.18_+0.01* 1.14+0.01* 1.14+0.0l* 1.14+0.01 1.05+0.01 1.10+0.012* 1.08+0.01* U23 U24 U25 G26 U27 G28 U29 C30 Table 3: A ut=a=ea gaen, - 1.07+0.01 1.25+0.02 1.18+0.03 1.14+0.002 1.10+0.000 1.11+0.01* 1.05+0.01 1.10+0.01 1.12+0.01 1.13+0.01 1.14+0.01* 1.10+0.001 1.24+0.01* - - dacatn ratz CfQ/Cs and C, ef the 30-ntRNA at 298K Resick, for uoib no d not be amazd due to ronane ozerap. In arses, heeK (i'e - 29.05+2.19 26.10+1.09 21.41+1.79 1.08+0.01 1.08+0.002 ere no dupicate rmswent byanasensk), anenvr cf1% (0.01) hasben assuwid 102 dts ae has beencaied out for thex Chapter 3: RNA Tetraloop Dynamics R 2 [s] R1 [s'] G1 G2 C3 A4 C5 c/c8 2.07+0.10 2.24+0.06 2.84+0.10 2.24+0.03 2.89+0.18 U6 C7 U8 G9 G10 UlI A12 U13 C14 A15 C16 G17 G18 U19 A20 C21 C22 U23 U24 I, CC 1.61+0.02 1.59+0.01 1.62+0.01 1.50+0.01 1.52+0.01 6 /C 8 HetnOe C1 , I 14.98+2.94 17.95+2.89 17.78+3.14 16.20+0.81 19.84+6.73 15.07+0.85 1.20+0.003 15.30+0.48 1.16+0.01 15.38+0.49 1.08+0.01 15.99+0.36 1.10+0.02 16.15_+0.65 1.11+0.03 1.17+0.01* 1.15+0.01* 1.11+0.01* 1.14+0.004 1.08+0.01* 15.17+0.61 15.06+0.33 1.11+0.02 1.08+0.01 - - 1.58+0.01 1.57+0.01 1.60+0.01 1.56+0.01 18.07+3.05 20.31+1.35 19.73+4.60 21.50+7.32 20.94+1.69 15.74+0.69 20.52+0.80 18.27+3.46 10.29+0.37 17.05_+2.25 15.10+6.09 12.06+1.94 19.72+1.66 14.93+0.81 19.60+4.10 20.22+3.52 1.1+0.01* 1.17+0.01 1.12+0.01* 1.07+0.01* 1.13+0.003 1.21+0.002 1.17+0.01 1.12+0.01* 1.23+0.01 1.18+0.01* 1.14+0.01* 1.14+0.01* 1.1+0.001 1.07+0.004 1.1+0.01* 1.08+0.01* 1.67+0.01 20.31+1.26 14.05+0.35 .. 2.66+0.09 2.85+0.04 2.20+0.08 2.40+0.11 2.80+0.05 2.27+0.02 - 2.87+0.12 1.92+0.02 2.78+0.08 2.24+0.23 2.38+0.07 2.84+0.05 2.33_+0.03 2.74+0.12 2.82+0.11 . . 2.81_+0.04 1.57+0.01 1.55+0.01 1.56+0.01 1.63+0.01 1.61+0.01 1.66+0.01 1.74+0.01 1.87+0.03 1.76+0.02 1.91+0.01 - 15.39+0.58 1.10+0.01 15.79+0.37 1.09+0.01 15.20_+0.37 1.12+0.01 15.23+0.37 1.16+0.003 15.27+0.54 1.12+0.001 11.33_+0.78 1.22+0.01 14.25+1.18 1.11+0.004 18.07+0.61 1.16+0.17 1.17+0.01 15.89+0.39 1.12+0.002 14.90+0.38 111+0.002 13.69+0.54 1.13+0.002 15.82+0.57 1.08+0.01 1.12+0.01 U25 G26 U27_ G28 U29 C30 C1 , G6 /C 8 1.2+0.004 _. 2.35 +0.09 2.30_+0.07 2.85+0.04 2.66+0.10 - 1.51+0.01 1.54+0.01 1.51+0.02 14.67+4.05 - 20.00+4.70 15.66+0.59 1.09+0.02 19.81+1.54 16.75±+0.45 1.10+0.004 20.58_+3.10 13.00+0.94 1.10+0.03 1.11+0.01* -. 1.14+0.01* 1.14+0.004 1.24+0.012 Table 4:A torvrai daxai ratesf C/C andC, ofe 30-ntRNA at 317K Reidus,for ubh n rnemts are g wm ld n beandyeziddw to wmame o*dap. In ases, teren dicate rnasurent h ben aied aztfor the betne (iri'amd byan astesk), ane r'rof1% (0.01) hasbeenass 103 i Chapter 3: RNA Tetraloop Dynamics I Pe I Kip I "7 0 .. C _C ! I 0 1 0.5 [ 0 1.5 I 0.1 0.05 0.15 TM [s] [ U7, G9 and G12 qe 14-ntRNA rdxazdan deatyaaus fC and Qfr res 11:R (ft) and R1p(nright) dday . Theaus epet nmapwid at 298K The le heits (in arbary wits) areplot agmrt tenxati Figur 2-paranrzerfits. Tk dqlite in de gra&. data sets, eh hw ben acq pak in Oierto otain emm fordie mties, are ilm Figure 12 shows the relaxation data for both C6/C and C. of the 14-nt RNA at 298K. These data demonstrates two general characteristics of the measured relaxation rates: - R1 as well as R2 relaxation rates of C6of both cytidine and uridine residues are systematically higher than C8 relaxation rates in guanine and adenine. On average, R1 is 20%, R 2 30% higher for the C6. - R and R2 relaxation rates of C1. are smaller than aromatic carbon relaxation rates. On average, they amount to only 63% of the respective C6 values. A possible explanation for the increased relaxation rates of C6 in pyrimidines could be the presence of a second dipole, C, in the vicinity, while C8 in purines represents a more isolated I-S spin system. However, as discussed in detail below, the effect of the CCdipolar relaxation is too small to account for the observed -30% difference in relaxation rates between C6and C. An alternative explanation could be found in the difference in CSA values of C6 and C. Since the CSA constitutes one of the two main sources of nuclear relaxation, differences in its magnitude are likely to be relaxation relevant. 104 - - - Chapter 3: RNA Tetraloop Dynamics A B 1 29 6 .'4 1 lb 6 3 47 12 . m 4I 12 35 9 1 2 - Il W 0 20 20 I 8 13 4 .to 2 2 ; 20 '15 15 10 n 5 iiii 0 0 1.5 1.5 01 D 0.5 0 04 12 9 012358131467 Al G C 1 0oc 0.5 I0 0 X 4 I1 C8 C6 0 12 3 5 8 13 C - I ,I~~~---- 1 2 9 A I1 U G _ l . U _ I C 1. Figure 12:MeasuredR,R2 ardtnC 6Q/Cs (4 and Ci' (B) f de 14-ntRNA stad y hase Reside mins aregin dandabneo degraPfs.Thelop riess arelabe indrk e o es e daing basepairin lit gry Two studies on 13C CS-tensors in nucleotides are available to date, one based on 13Cchemical sift components determined by solid-state NMR experiments in combination with density functional theory (DF) calculations [26] and one exclusively relying on DFT calculations [25]. While these two studies agree to a varying degree for the different nucleotides (Table 5), the most remarkable difference is that while in ref. [25] similar CSA values are proposed for C of the two purines as well as for C6 of the two pyrimidines, ref. [26] agrees on the similarity of the purine CSA values but reports a CSA for cytidine, which is about 40ppm lower than the one for uridine. . CSA [ppm] Adenine Guanine C6 Cyddine Uudine Table 5: CSA r. [26 ref[25] 131.4 139.6 156.8 195.5 122.8 119.0 183.9 184.1 esforC6ad CGami toFiala etaL [25andStuer 105 etaL [26]. Chapter 3: RNA Tetraloop Dynamics As shown in Figure 13, R1 and R2 increase by about 30% for a molecule the size of the 14-nt RNA, when the CSA is increased from 120 to 185ppm, signifying that this difference in the CSA can indeed fully explain the observed difference between C6 - and CQ-relaxation rates. Furthermore, the similarity in the observed relaxation rates for cytosine and uridine residues indicates that the (CSA values determined in ref. [25] reflect the CSA in oligonucleotides more closely than the ones from ref. [26] and should therefore be preferablyused in the further analysis. From Figure 13, it becomes also clear that errors in the absolute CSA are more dramatic for larger CSA values, hence more crucial for C6 and C than for q. C1 The CSA of C1 is about 45ppm in C - erdo conformation according to ref. [25] and 30ppm for Cq-erdo and 60ppm for Q,-edo as reported in ref. [57]. A B 7 70 6 60 5 50 X O: 3 : 40 30 2 20 1 10 0 0 0 2 4 6 8 10 0 2 4 t, [ns] 6 8 10 T= [ns] C z 00C 4- 1.5 I 0 2 4 6 8 10 · [ns] Figure 13: 3C CSA aWtibthon to 13C awda daxation R1, R 2 and theheC haze beencadatd peig on r, cth an assurd CSA of Oppt 30Cp 60ppn 120ppmand 185ppmat a field strth of 600 MHz. The GH int ar wtor nth ws set to 1.09A. The aation ti f the 14-nt and the30-nt RNA at 298Kare iit 106 Chapter 3: RNA Tetraloop Dynamics Even if a CSA of 60ppm is accounted, R and R2 of C1, arrive at only 68% of the respective values calculated with a CSA of 185ppm, which corresponds to the observed differences between C1 , and C6 relaxation rates. Hence, the lower CSA of the aliphatic as compared to the aromatic carbons fully accounts for the smaller R 1 and R2values of C 1, compared to C6 and C. 3.3.3.2 Model-free analysis In order to assess the validity of the desired residue specific dynamics obtained from the modelfree analysis, the global parameters extracted in the process, the diffusion tensor and Tc, have been compared to those derived by independent means. Furthermore, as demonstrated above, the important external parameter for the analysis of "3 C relaxation data is the two available sets of 13 C CSA 3C CSA. Therefore, the values from ref. [25] and [26] have been compared in their potency to produce a sensible output of the model-free analysis. Only after these methodological investigations, the actual dynamic interpretation has been carried out. The CCGdipolarcontribution to C6 and C1 relaxation - The model-free formalism has been developed for an isolated I-S spin system. While it can be readily applied to investigate C in purines, C6 in pyrimidines and C1, both possess a neighboring S-spin (C or C2.), which contributes to relaxation through a CCdipolar mechanism The contribution of an additional CCdipole relativeto the dipolar relaxation caused bythe directly bound proton is expressed in Eq. (15) [58]: 3 rC 1 ~(1)S~ ~PHC Pcc crcH I°c in which Pic is the dipolar contribution to the relaxation of the 13C nucleus arising from the attached H or "3 C nucleus; i is the gyromagnetic ratio of nucleus i; r is the distance between the spins i and j; ac is the carbon Lamor frequency and T%is the overall rotational correlation time of the molecule. The relative CCdipolar contribution of C6 and C2. to the relaxation of Co and respectively, is depicted in Figure 14 in dependence of the overall rotational correlation time 107 Tc. C1., Chapter 3: RNA Tetraloop Dynamics 4 C5 -C6 3 I0 a 2 - C.-C 2 I Q 1 0 0 2 6 4 8 10 TC [ns] Figuw 14:CDian the oerd all ae CGCidar aw to CH-dar mhanism to erdaxcation qrfC6and Cl in deewe nt qr the intse wndation tm t as dzoaidl inEq. (15). The stmtural arra ad f dxeac4amnt ti frtfhe 14-rtand 303ntRNA at 298Kae irkitL A field carbonspim(gey dis) is sho iinc)tdiG C sttp_ f 600MHz has en assut1 The irenmdrdistn fir GH, C1-C2' and C6-Cshawe bn set to 1.09a, 1.53A ard1.37A as traatdfrnINSIGHTII(nim. In addition to the dependence on the nuclear magnetic susceptibilityand the sixth power of the internuclear distance, the GCdipolar contribution increases with the square of both the correlation time and the magnetic field strength, signifying that the CGdipolar contribution becomes more notable for larger molecules as well as at higher fields. Due to the dependence on the gyromagnetic ratio as well as the sixth power of the internuclear vector, the CCq-dipolar contribution to C6 relaxationis only about 1% of the CH-dipolar relaxation for a molecule of the size of the 30-nt RNA (=5.65ns at 298K) and even smaller for the 14-nt RNA (c=1.92ns). Sincethe C.-C 2. bond vector is longerthan the C6-Qvector (1.53as compared to 1.37A),the C2 Cdipolar contribution to C, relaxation amounts to only around 0.5% for the 30-nt RNA. Taking into account CSA relaxation, the CCdipolar contribution to overall spin relaxation is even smaller. Therefore, for both C1 and C 6/CG, the C dipolar contribution has been neglected in the dynamic analysis of the molecules investigated in here and CqH1 and C6 H6 have been treated as I-S spinsystems. 108 - - Chapter 3: RNA Tetraloop Dynamics The Diffusion Model - The program Modelfree [55] consistently fits the combined C1,and the C/C 4 relaxation data of the 14-nt RNA to an axially symmetric diffusion model with its unique principal component oriented along the helix axis and an anisotropy (D= 1/) of 1.33 at both temperatures (Figure 15A). The axially symmetric diffusion model constitutes the most complex model contained in the Modelfree program. Size and orientation of the diffusion tensor determined by Modelfree have therefore been cross-validated by hydrodynamic calculations using the program hydroNMR [56]. The tensor determined by hydroNMR is axially symmetric with its orientation within 5 identical to the Modelfree results with an anisotropy D=/1 1 of 1.39. Both tensors are in agreement with an earlier dynamic study carried out on the 14-nt RNA based on 15 N relaxation rates [59], where an anisotropy of 1.34 has been determined. B A df sideziwarndtop ew The 14-nt(4)ard e30-ntRNA (B) demiinM Figure 15:Dfiin temorqcfdhe dfsian tenor f the 14-ntRNA is gizeningmyin mearfranrfe30-rtRNA. For the 30-nt RNA, a diffusion anisotropy of 1.81 is fit from the relaxation data (Figure 15B). This is validated by the hydrodynamic calculations, which arrives at an axially symmetric tensor with an anisotropy of 1.9. The principal tensor component is again similar within about 5° for Modelfree and hydroNMR It has to be noted that while for both the 14-nt and the 30-nt RNA, the principal 109 Chapter 3: RNA Tetraloop Dynamics diffusion tensor component is oriented along the helix axis, due to the longer stem of the 30-nt RNA, they are tilted about 40 ° away from each other (Figure 15). This indicates that the C-H vector orientation relative to the diffusion tensor is not the same in every RNA even for the vectors in the planar base, but depend on the size of the RNA. The effect of different diffusion models on C6 /Ca and C,1. relaxation rate analysis is shown in Figure 16. The outcome of the model-free analysis on the 14-nt RNA with an isotropic tumbling model is compared to the same procedure using an axially symmetric diffusion tensor. In the second case, the relaxation rates depend on the orientation of the GH vector with respect to the diffusion tensor. While for the relaxation properties of C6 and C8 (Figure 16A), the diffusion model has almost no effect on the stem residues, it affects residue C8 and to a lesser extent also G9. For C1., (Figure 16B), most of the stem residues are also not sensitive to the diffusion model, only the terminal residues 1 and 2 and the loop residue 9 show differences to the isotropic model. It is remarkable that in all deviating cases the isotropic model results in a more flexible S2. A 1 270 0.8 180 N C 0.6 90 0 0.4 1 2 3 4 5 6 7 8 9 10 11 12 13 14 Residue c1. B 270 1 Isotropic 0.8 Anisotropic 180 ea . 0.6 . . v G G C A C U - ,. i I . . 1 2 Figur 16:Effects o the dfi nGon 3 4 90 !.o' L,, fnA . . U C GG . . U G C C . . . . . . - 5 6 7 8 9 10 11 12 13 14 Residue the rxed-fimarlysis. C6/C8 (4) arndC' (B) S2 parantes Al ,axation data f the 14-rt RNA at 298K sing an i mti: (g'y lie) or an anis si axy snD ifrm the (Hk irms) gn aaateda dfion nmi Theark 0 Qeetuntherpectie GH wts andtheprnzipleaxis f thediwon tenoramre yM oddfire (dashac11l). 110 Chapter 3: RNA Tetraloop Dynamics The relative insensitivity of the stem as compared to the loop residues to the diffusion model can be understood when considering the orientation of the respective GH vectors relative to the diffusion tensor (see angle 0 shown in Figure 16). In stem regions of RNA molecules, the diffusion tensor is oriented about perpendicular to the base planes, resulting in angles 0 with the principalaxis of the diffusion tensor of around 90 ° for C--H 6 and C-H 8 vectors. Since RNA is in addition almost axially symmetric, the orientation of the GH vectors within the base plane does not affect their relaxation properties. Hence, the relaxation behavior of all base paired residues can be expected to be similar. Furthermore, the relaxation properties of vectors perpendicular to the long diffusion tensor axis is governed by rotations around the principal axis, while it is less sensitive to rotations along both other axes. Incidentally, rotations around the principal axis occur more often, signifying that vectors perpendicular to the long diffusion tensor axis and hence for RNA vectors in the base plane will be less sensitive to the applied diffusion model as vectors parallel to the long axis. In contrast to the C-H 6 and C-H48 vectors, the angles 0 between C H1 . and the diffusion tensor axis are more diverse (Figure 16B). In line with this observation, the Cq, data alone results in a similar diffusion tensor, while the C6 /C4 data alone fits to an isotropic diffusion model. This analysis shows that even for a molecule as small as the 14-nt RNA with an anisotropy of 1.33, anisotropic diffusion affects the resulting dynamic parameters, especially in the most interesting loop region, in which the C-H vector orientations deviate from the ones in the stem region. These deviations are, however, only defined, if the molecule under investigation is structurally characterized. It follows that while anisotropic diffusion has to be included in the dynamic analysis in order to dissect structural and dynamic effects on the observed relaxation rates, the inclusion of a molecular structure introduces an additional potential source of error. The overall rotational correlation time c - The overall rotational correlation times determined by different means for the 14-nt RNA at 298K and 317K are given in Table 6. rc,[ns] 298K M aydfiwbA oNMR C6/C 1.92 2.47 R2/R, 1.72 ModfE b mNMR 1.31 1.62 1.89 C, Table 6: rc w1ue frdx 317K 14-rntRNA. The zc resdingfmheanraediR 111 2 /RI R2/R1 1.58 1.42 ratio rfalldJiestemresid Isgwn Chapter 3: RNA Tetraloop Dynamics Correlation times of 1.92ns and 1.31lns at 298K and 317K, respectively, have been obtained from the extensive model-free analysis for the combined C 6 /CQ and C1 , relaxation data. While at 298K, these value is slightly higher than the approximate values determinated from the R2/R1 ratio of all T, C1 it is slightlylower at 317K (1.58ns for C6/C 8 the stem residues (1.72ns for Cq/C and 1.89ns for Q), and 1.42ns for C1 ). The T, values from the hydrodynamic calculation are about 0.6 and 0.3ns higher than the model-free results at 298K and 317K, respectively. In spite of these deviations, the correlation with tT/T, the ratio of the viscosity at a given temperature and the temperature is linear for the relaxation data derived x, values (Figure 17A). In an earlier 15N relaxation analysis conducted on the same 14-nt RNA at 273K a c of 5.7ns has been reported [59]. This value is in better agreement with the hydrodynamic calculation than the 13C relaxation analysis. A B 6 6 5 5 4 in 4 U) 3 LI 0 19 2 3 2 1 1 0 0 0 3 4 5 6 2 T/T* 105 [gm*cm'l*sec1*Kl 7 1 0 ] 1 2 3 qT/T*10 [gm*cm'l*sec'l*K1] Figur 17:Depeder q r, on e ratioaee thezsaity fuaterand a dute dxe13C ndSxatn data uiig Malief 30-nrtRNA (B). rchas ben deUermum erawfrr e 14-rt(4 andt at 298K and 317K (dark grey the Ised Tn nic caa u ing dianods), fan "15N iaxatzondata [59] at 273K (bade dot),firm sane pmgramAbdrNMR (litgrey sqmmar) andfim e separate R2/Ri rats jCV C andCQ(Hak andagly M I ). 7he lio mpment the Itliarfit to e nfxId-fie (blaxk In) and d e7)dNMR 112 data(Ivy=1) 4 de ongm Chapter 3: RNA Tetraloop Dynamics For the 30-nt RNA (Table 7), the c of the model-free analysis (5.65ns and 3.65ns at 298K and 317K) are about 0.65 and 0.45ns higher than the xc values of the C6/C8 R 2 /R 1 ratio and about 0.2 and 0.6ns lower than the C, R2/R1 ratio. Also for the 30-nt RNA, the dependence of the model-free results on temperature is linear (Figure 17B). r,[I] 298K Mcdfm C6/8 Qi/S _ NMR 5.65 3.67 _'__ Table Z7:rC 317K /R1 eRAdoNMR 4.98 6.18 3.65 2.40 R2/R 3.19 3.83 fifrthe3O-ntRNA. Although the reason for the differences between the experimental and the theoretical c cannot be elucidated in here, the linearity of the xcversus T/T relationship for both the 14-nt and the 30-nt RNA establishes confidence in the model-free relaxation data analysis. This data demonstrates that c obtained from the R2 /R1 ratios of C1. reflect the actual values better than the one from C/C 8 . The C chemical shift anisotropy - Model-free analysesof the C6 /C8 relaxation data obtained on the 14-nt RNA using either the 3C CSA values taken from Fiala et al. [25] or from Stueber et al. [26] (Table 5) are shown in Figure 18A. If Stueber et al. CSA values are used, the average stem S2 values are around 0.8-0.85 for all nucleotides but uridine, while S2 for the only stem uridine, U11, is significantly higher (close to 1). In addition, U6 in the loop shows an elevated S2, suggesting that this residue is more stable than the stem residues. For the 30-nt RNA, all stem uridines exhibit higher S2 values than the other residues, too (data not shown). In contrast, if the (CSA values from Fiala et al. are incorporated, the uridines exhibit similar behavior to the other nucleotides. Furthermore, the fits of the model-free parameters to the uridine relaxation data are improved in every case. As mentioned above, the main difference between the two sets of CSA values is that while Fiala et al. calculate similar values for C8 in both purines as well as for C6 in the two pyrimidines, Stueber et al. report similar values for C8 but a C6 CSA value for cytosine that is about 30ppm lower than the one for uridine. 113 Chapter 3: RNA Tetraloop Dynamics A C 6/C 8 I r-'T] Fiala ,,'" -r.".' 0.8 .-,-"---e * tal. Stueber et al, N cn 0.6 stem > C~U G G C A T. '.. ' . .. .. 1 2 3 4 5 6 0.4 _. loop U .. r. 7 8 stem C 11 G. . " U . . .. . . . 9 10 11 12 13 14 Residue C1. B I l- . so 0.8 '60-60 stemlopse Nc U) 0.6 0.4 GG CA C UUC GGUGC C 1 2 3 4 5 6 7 8 9 1011 121314 Residue Figure18:Effecf theCSAonteS2 w mukgfmtenrdd-friansis f te 14-ntRNAat 298KA C/C caladted the CSA Vduesfi*nStu r et aL[26] (gy dianmrs arndlies) andFialaetal. [25] ('ade), the3 urci reii a rd bes. B S2 wh alt uQ a CSA ef 30pmfor al rmsdz (gay) r a CSA 30ppmfor all ids in Cy-e3domzfomtiw (1-6, 9-14) and 60ppmfor U7 and C8 (ade), hih are in C2'-end S2 Vue Since the R1 and R2 relaxation rates observed in the stem uridines are simnilarto the ones of the stem cytosine residues (see Figure 12), and there is furthermore no apparent reason for an increased stability of the uridines, the further analysis has been carried out with the values provided by Fiala et al.. However, for both sets of CSA values the order parameters of the cytosines are lower than the S2 of the other residues (Figure 18). This is also observed for the 30-nt RNA (see Figure 19). While this could signify that the bases of cytosines are in general more mobile than the other nucleobases, it is not reasonable to assume that cytosine, which is in a three hydrogen bond Watson-Crick arrangement with guanosine would be more flexible than uridine, which forms only two hydrogen 114 Chapter 3: RNA Tetraloop Dynamics bonds with adenine. It follows that the GSA for C6 of cytosine is most likely actually lower than it has been reported. Figure 18 illustrates the effect of using GSA values, which deviate from the actual CSA. If the assumed CSA is lower than the actual one, the resulting S2 value indicates a more rigid behavior and vice versa. The error propagated into S2 is higher for C6 and C (Figure 18A), which exhibit higher absolute CSA values than for C1r . For C 1 , the CSA has been reported to be ribose pucker dependent [57]. Figure 18B demonstrates the difference in S2 for CQ,using an assumed GSA of 30ppm as compared to 60ppm for residues U7 and C8, which are in C2,-endoconformation. For the higher CSA value, S2 decreases by about 0.03ppm in both cases, indicating a more flexible behavior. The increased flexibility of these two residues is, however, also apparent, if a CSA of 30ppm is used. 3.3.3.3 Dynamics of the 14-nt RNA The results of the model-free analysis of the 14-nt cUUCGg hairpin at 298K and at 317K are summarized in Table 8 and Table 9. Some of the relaxation data could not fit satisfyingly to any of the dynamic models (grey shaded data in Table 8 and Table 9). In these cases, the results of the model-free analysis using the simplest model (Model 1, Figure 7A) are given. In the following, the dynamic behavior of Cq and C8 will be considered as a dynamic reporter of the entire base moiety, while C1., dynamics will be treated as reflecting the flexibility of the whole ribose moiety. At room temperature, all base relaxation rates but the one of U7 can be fit with the simplest model, signifying the absence of slow internal motions (S 2 1) as well as slow exchange processes (R- =0) and the presence of onlyvery fast internal motions (=t--e -0). The relaxation behavior of the U7 base moiety is more complicated in that it exhibits millisecond exchange (Rex=2.14s-1). At 317K, more residues show slow dynamics and 17 acquires fast time scale motions in addition to the slow exchange process. For the ribose moiety, most residues can be fit with the simplest dynamic model, only G1 requires a small fast time-scale motion term (Te=7 .4 2 ps) at 298K and at 317K G10 acquires a R term (Rex=2.74s-1). 115 Chapter 3: RNA Tetraloop Dynamics Base S Ribose [ps] 'rTep]| s | G1 G2 C3 A4 C5 0.85+0.01 0.78±0.05 0.87+0.02 0.83+0.01 0.86+0.01 0.83+0.01 0.88±0.01 0.82±0.01 0.88+0.02 0.83+0.01 U6 0.87+0.01 0.84±001 U7 C8 0.67+0.01 2.14+0.67 | R. [s ] [ps] T 7.42+4.05 _ 0.77+0.02 0.84+0.01 0.73+0.02 G9 0.83±0.01 G10O 0.89+0.01 Ull 0.91+0.01 G12 0.91:t0.01 C13 C14 0.86+0.02 0.83+0.01 0.85+0.02 0.80+0.01 0.81±0.01l : 0.80+0.01 _____ - 081±0.01 .. 0.82±0.01 _ T=298K; xc=1.92ns, D=-1.33 Table 8:Results f the r l-fiearsis for C6/C8 ('Base' and C'(Rikaeq ctfe 14-ntRNA at 298K The grey sladMdata wd not befit toanmy dym cnxd win the O.05to 0.00 crtical Base S G1 0.77+0.02 G2 0.81+0.02 [ps] |Te[p]|'r Ribose 1 [ps] s 0.83+0.02 0.86±0.01 3.77+0.58 C3 0.78+0.002 0.88±0.01 A4 0.82+0.02 0.87+0.01 C5 0.80+0.02 0.88+0.01 U6 U7 0.82+0.02 0.87±0.01 C8 0.77+0.02 0.58+0.01 | R [s'] 10.16+2.66 2.16+0.49 _ 0.78+0.01 0.80+0.02 G9 G10O 0.75+0.02 Ull G12 0.83+0.02 0.83 +0.02 C13 0.80+0.02 0.87+0.01 C14 0.80+0.02 0.79±0.01 1.46+0.48 0.84+0.01 0.81+0.02 0.84+0.01 2.74 ±0.63 0.87+0.01 0.86+0.01 2.11+0.55 T=317K; TC=1.31ns; D =1.33 Table 9: Resultsof the nmxde-fiee amys is for C6/C8 ('Base') and Cl' (Ribe) f tde 14-nt RNA at 317K The greyshadeddata acd not hefit to any dynmic mnIeld i te 0.05 to 0.00 acitid udue 116 _ . . .. .. , _ . . Chapter 3: RNA Tetraloop Dynamics ~298K ~4 I. ^V +/ . 0.8 N -::~...:..:. ..'~: :.-..:'.".. . 0.6 G .... ,;-; .- ..... .\ {,.4s.::.-....:.. ... Ft~~ibose . ',,,-1'' ''.':...''' ^,'..-'.,,''-.'' ' ':. GGC 3 4 5 ,"' ' ~.' '- C G'G ACUU 2 1 '" ''.- 6 7 8 C2 .- endo -10 . ...'..'...'-:,'--..- ~... .. . C-. ;-.'.''.-....'-. .:.;,. . ' ' .:.-. .;... :i ,'u ' .,:.,.:. ,~.;,"."'-....-., ....::.:. ,.t: :~....... . lA- +~~Ba '" ........ -.....- -5 , N .. -r' ,_, - N Ca - ':. ... UG C C 9101112 O 1C 3 -endo C3.-endo 13 14 Residue 317K 1-- Ribose 0.8 - - ";'A '' * cm: CDU.: . \ / Base i .'.''"'''''''''"'" .:..'\i.';."!.')'-:. "'''' "..'.:.':':-':?. .. ................. :." ...{' -:-'-.'' 0.6 1 . .'5 G C A C U U C G G U! ~G C~ C ~~~ I I I I I I I I 1 2 3 4 5 6 7 8 I I 9 1011 I . 10 i:!-............... . '.. .. :'...--............ '~~~~~~'.' ' . '-...,..'..'-.. :- - ' . : .:-.:.:.. '. ....'. -'b'.'--,'.:-.~. 0.4GG C2.-endo 152 I 5 . ". -rOI'....... ~.endo CC 3 -endo II 121314 Residue Figur 19:S2paramrtesfor C6/C8 ('Base', a sdid lies) and Cl (Ribse' gey solid line)f the 14-ntRNA at 298K (ahoz) and317K( o. For thedlo and the w a4arenues, 3J(Hr,H29)clg costnts aregienfpossible(a dashed la). S2 values for the base and the ribose of the 14-nt RNA at 298K and 317K are shown in Figure 19. From these order parameters, the following observations can be made: At both temperatures and for the base as well as for the ribose, the stem residues except for the terminal ones exhibit very similar dynamics. Thus, the average S2 for the bases in the stem is 0.88 117 ' Chapter 3: RNA Tetraloop Dynamics with a deviation of only 0.003 at 298K and 0.81+0.006 at 317K. For the ribose, the stem mobility is even more uniform with 0.83 +0.001 and 0.87 +0.001. While the overall S2 pattern across the sequence is remarkably similar at the two different temperatures for both the base and the ribose, the flexibility increases at higher temperature for the base but decreases for the ribose. A possible explanation for this contrary temperature dependence could be found in an entropy compensation mechanism. Below the melting temperature, an increase in base flexibility cannot be compensated enthalpy-wise, but has to be compensated entropically by decreased ribose flexibility. 3J(H11,H2.) coupling constants are in agreement with an increased rigidity of the ribose moieties at higher temperature (Figure 19). For the loop residues U7 and U8, which are in 2 .-ei ribose conformation, 3 J(I-H.,H ,) 1 2 values are large. Upon temperature increase, these coupling constants increase as well, indicating an even more rigid conformational arrangement. In general, the similarity in the dynamic profile along the sequence at the two investigated temperatures signifies that although the overall flexibility changes, no significant difference in the dynamic behavior of any specific residue occurs. This confirms that the cUUCGGgloop is stable at 317K. In addition to its structure, also its flexibility does not change within the investigated temperature range. In particular, the dynamics of the cUUCGg motif are discussed in the following: In this, the dynamics of the loop residues are interpreted in reference to the stably base paired and stacked stem residues, which are considered rigid. Whereas the bases of U6 and CS are as rigid as the stem residues and the one of G9 exhibits only slightly increased flexibility (S2 =0.83 at 298K), the base of U7 is significantly more flexible (S2 =0.67). In addition, the ribose moieties of U7 and C8 are flexible but to a lesser extent. These observations are in agreement with the reported structure of the cUUCGg loop. The flexible base of U7 has been reported to be the only one, which is not stacked but protrudes into solution. Furthermore, neither flexible ribose is involved in hydrogen bonding. Although in general the dynamics do not change at higher temperature, the flexible base of U7 becomes even more flexible in respect to the rigid ones. The S2 of this moiety decreases from 0.67 at 298K to 0.58 at 317K. Thiis gain in flexibility is accompanied by a change in the dynamic characteristics in that the fast internal motions show a slightly slower time scale ( < 10ps at 298K; 10ps at 317K). This is in agreement with a larger amplitude of the internal motion. At both temperatures, the closing base pair of the cUUCGg loop exhibits dynamics similar to the stem base pairs, indicating a rigid arrangement. 118 Chapter 3: RNA Tetraloop Dynamics 3.3.3.4 Dynamics of the 30-nt RNA The model-free results of the 30-nt uCACGg RNA at 298K and 317K are summarized in Table 10 and Table 11, respectively. As for the 14-nt RNA, most of the residues can be fit to the simplest dynamic model at 298K, indicating an overall low extent of internal dynamics. The only truly flexible residue at this temperature is A15, the second loop residue. Both the base and the ribose moiety of this residue exhibit a complex dynamic behavior comprising fast internal motions at two different time scales. The similarity of the spatial restrictions (S 2 =0.63 +0.02 and 0.67 +0.06 for the base and the ribose, respectively 9 7 2 +193 ps S ,2 =0.82+0.02 for both moieties) as well as the time scales (e= 6 07+60ps and for the slow motion of the base and the ribose, respectively e < 10ps for the fast motion in both moieties)in the two moietiespoints to a concerted motional behavior of the whole residue. At higher temperature, the base but not the ribose moiety of residue A15 experiences an increase in flexibility. Remarkably, the model-free analysis allows to attribute the gain in flexibility exclusively to a change in the slower motional process, which becomes less restricted (S 2 drops from 0.63 to 0.58) and slower in time scale (e increases from 607 +60ps to 750 +147ps). Apart from A15, a number of residues, which are not flexible at lower temperature, show dramatically increased dynamics at 317K. At this temperature, the base of A12 constitutes the most flexible moiety of the 30-nt RNA. Interestingly, it exhibits extremely unrestricted motions (S2 =0.46) on a very fast time scale (e< lOps). Apart from that, this base moiety experiences millisecond exchange processes (Rex=6.4s-). In addition to the base also the ribose of A12 becomes more flexible at higher temperature but to a lesser extent. Albeit small in amplitude, this moiety shows motions on two time scales. Furthermore, the base of G18 in the loop closing base pair exhibits fast dynamics on two time scales.Although the extremelyslow time scale of the slower motion and the high error of it (1800ps ±670), does not seem credible by itself, the relaxation data can only be fit with this model, indicating that the presence of two motions is valid, even if the precise time scale is not. Unfortunately, due to lacking experimental data, no information about the ribose of G18 is available. Apart from these residues close to the apical loop, also the ribose of U25 in the distal bulge of the 30-nt RNA shows increased dynamics. 119 Chapter 3: RNA Tetraloop Dynamics Ribose Base _, ~ 2 S 2 Ss 222 S. G1 0.89+0.02 G2 0.87+0.01 C3 0.81±0.02 A4 0.84±0.01 0.84±0.02 0.89+0.01 Ss2 S Te [ps] |Re [S- 1] 0.73+0.02 11.92 ±4.47 8.63+1.60 0.79+0.01 0.90+0.01 6.38+1.98 C5 0.86+0.02 U6 C7 0.86+0.01 U8 0.85+0.01 0.82±0.01 G9 G10 U11 A12 U13 0.85+0.01 0.76+0.02 0.85 0.01 0.91+0.01 0.87+0.01 0.88+±0.01 0.87+0.01 0.90+0.02 0.78+0.01 3.98+1.98 0.93+0.02 0.84+0.01 C14 0.83+0.01 A15 0.51+ 0.02 0.81+0.01 C16 2 S2 Rex [S] Te[ps] 0.92+0.01 5.40+1.97 0.63+ 0.02 0.82+ 0.02 607.1+ 59.97 0.55+ 0.07 0.87+0.01 G17 G18 0.93 +0.04 0.96+0.01 0.87+0.01 0.86±0.01 U19 0.83±0.01 0.89+0.02 A20 0.86±0.01 0.78+0.02 C21 0.81+0.02 0.94+0.01 C22 U23 0.850.0l 0.89+0.01O U24 U25 G26 U27 G28 U29 0.83o+0.01 0.89+0.02 C30 0.780.02 0.67+ 0.06 0.82+ 0.07 ______ ______ 972.31+ 192.59 _ 0.82+0.01 0.95+0.03 0.83±0.01 0.82+0.01 0.85+0.01 0.89+0.01 0.85+0.01 0.97±_0.02 -______ 0.83+0.02 -________ + _____ ___________ 15.04 ±2.53 T=298K; tc =5.65ns; D =1.81 Table analysis of the 30-rnt RNA 10: Results of the nmSdel-fimee . aralyzeddue to reoane oear at 298K Residues, for ico res ults are gizen, cw not be Thegreyshadd data awddnot befit to any rrndl zithin the 0.05 to 0.00 critical iues. 120 Chapter 3: RNA Tetraloop Dynamics Base S 2 Ribose te[PS] 2 S PS-] Rex[] S2 G1 0.74+0.03 13.26+2.93 G2 0.79+0.02 6.73+3.23 C3 0.76+0.02 0.83±0.01 A4 C5 0.81+0.01 0.80 0.78+0.03 0.81±0.01 C7 U8 0.74+0.02 0.79±0.01 G9 0.79+0.03 G10 0.99+0.03 0.80±:0.01 Ull 0.81+0.01 0.85±0.01 2.36+0.85 2 Ss S SS 2 [p] e[ps] R[s] Rex[S1 ] 0.74+0.01 2.95±0.86 0.76±0.01 2.26±0.51 ±0.01 U6 0.81+0.01 6.39+0.77 6.39+0.77 A12 _= 0.46+0.01 A-2 0-46±0.01 U13 C14 0.80+0.03 16.83+5.45 0.76+0.02 0.58+ A15 0.47+ C16 G17 - 0.82± 0.02 0.01 0.01 150.84 0.72± 0.03 0.84± 0.04 823.96± 180.04 0.88±0.01 0.85±0.01 0.75+0.02 0.77+0.03 0.87±0.01 G18 G18 0.53+ 0.06 0.02 0.71+ 0.03 0.81+ 0.05 0.74+ 0.07 750.19+ 147.18 0.80+0.01 0.80i±0.01 A20 0.83+0.01 0.78±0.01 C21 C22 0.78+0.02 0.83±:0.01 0.80+0.02 0.82±:0.01 U23 U24 0.81+ 0.75± 0.01 0.02 U25 - G26 0.73+0.05 U27 - G28 0.89+0.02 0.84 ±0.01 U29 0.81+0.01l 0.82±0.01 0.78+0.02 3.60 ±0.63 1843.14+ 668.08 U19 C30 0.94± 619.41+ 0.77± 0.61± 0.04 0.79±:0.01 0.03 1.66±0.37 0.76±0.01 4.16+0.95 0.80±0. 0.94±0. 727.51± 01 02 210.65 51.55+22.10 __ 0.72±0.01 1.6084 - ~~~~~~~~~~~~~~~~~~~~~1.60 T=317K; Tc=3.65ns;D=1.81 foruhich no dresuts aregiwenculd notbe Table 11:Resuts f tle rrd-fiee analysisf the 30-nt RNA at 317K Residues, arnyzed due to resonaxeozeap. Thegey shadl data dd rt befit toany rnrdelzuithin the 0.05 to 0.00 itical wues. The order parameters for the base and the ribose moieties of the 30-nt RNA at the two temperatures are depicted in Figure 20. The stem residues of both moieties exhibit in general similar S2 values. The only exception is the base moiety of G10, which has a highly increased S2. This is, 121 Chapter 3: RNA Tetraloop Dynamics however, not due to a bad fit in the model-free analysis since the relaxation data fits well satisfyingly to the simple Model 1. In contrast to the dynamics of the 14-nt RNA, the stem ribose moieties are on average slightly more rigid than the base moieties at both temperatures. Upon temperature increase, a concerted increase in flexibility is observed. 298K 1 ~..+..i , r..F , :/l,, * 0.9 _ ~I~ 0.8 ~,, . /.:. . Ribose Base 0.7 Jbulgp: I bulae u!o0.6 C2 .-endo 0.5 . q: 0.4 '"' ~. ' ~'": Yp'08-*1qs,."+;, i :.::':;-'-,:,ii ' .:.'~'.:i. =: ..:'.- ~''r'. .'.!:.'::''.:::-' ; .:.t";' 'i ': 0.3 0.2 ' . '-,-.',' .:..-= . ';-::..: ..r.:.-': .. ,,!:.:.': .'.:..... :' ',^,:1 .!...- .:i':::~~~~~~~~~~~~~. '"' ':.: ..i ::':: ' ''....,.;.'. :.i-'-::::!.'7! 1 0 ,.: ''.-:':i: ' :: ?;-." ,'.!.'.';}!; '",i~~".:i ;.:i: GGCA . UG . . . . ..C U UUGUG . . . UAUCACGG . . . . . . . . UAC . . C . UGG . . . CU **i. 2 4 6 8 X .:!';..' :..." 5 - IM Z- N X o 1d C .-endo 3 10 12 14 16 18 20 22 24 26 28 30 Residue 317K 1 0.9 0.8 0.7 N 0.6 Cl C2 .-endo 0.5 'N X ,-q 0.4 5 0.3 C 34-endo C.-endo n.2 ar v 2 Figu 4 6 8 10 12 14 16 18 20 22 24 26 28 30 Residue q the30-ntRNA at 298K C6/C8('Base';blak solidl) andCi'(ibse'; gysolid lines) stants aregizen fpssile(bak For de kp and dtetw a4antresidues, 3J(H,H2) awplzrga 20: S2parantefor (abhze)and317K (4oz. daisellui). 122 , . . Chapter 3: RNA Tetraloop Dynamics Thus, the mean S2 of the stem residues, which do not exhibit increased dynamics, drops from 0.85+0.07 to 0.77+0.06 for the base and from 0.88+0.09 to 0.81+0.03 for the ribose moieties. In agreement with these observation, the 3 J(H1.,H 2.) coupling constants for the two residues in the C 2 oz/o conformation, A15 and C16, remain the same at the two temperatures (Figure 20). Of the residues in the uCACGg loop, positions L1 and L3 exhibit completely stem-like behavior at both temperatures; L2 exhibits high flexibility both in its ribose and its base and L4 shows extreme rigidityin both the ribose and the base at lower temperature. At higher temperature, the base but not the ribose of this residue adopts increased flexibility to an extent of the average stem-like behavior. In conclusion, the overall loop dynamics exhibit only minor changes at 317K compared to 298K, signifying that the uCACGg loop structure is still intact at higher temperature. Although the loop structure remains unperturbed at 317K, the regions adjacent to it are subjected to dramatic dynamic changes. Thus, the base of G18, which constitutes one part of the closing base pair, and the base as well as the ribose of the adjacent A12 on the opposite strand exhibit increased flexibility.This demonstrates that while the actual loop structure of the uCACGg motif is still intact at 317K, the stem adjacent to it has started to melt. 3.3.3.5 Motional implications In combination with the imino proton line width data and the 3 J(H1 .,H2.) coupling constants, the 13 C model-free parameters can be used to construct a dynamic model of the two tetraloops studied in here. Translation of model-free parameters into defined motional models, however, has to be carried out under careful steric considerations concerning the possible modes of motion in a given system. Independent motions of the C-H 6 or C-H vectors in the internally rigid base moieties have to be due to rotations around the glycosidictorsion angle X. In this case, the GAF-model can be applied, which translates S2 into a rotation around the Cq.N axis (see Figure 9). Figure 21 shows the extent of motion involved in a rotation around the glycosidic bond by +15 in a canonical stem arrangement. In addition to the motionally independent bases, all those involved in base pairs have been modeled using the GAF-model. Since the flexibility of these moieties is thus considered to arise exclusively from rotations around the glycosidic linkage the overall extent of flexibility might be overestimated. 123 Chapter 3: RNA Tetraloop Dynamics Figue 21:Fca C B A an.i'. AC -fomRNA ° .m Bnym?';B& ' 15 dedat In contrast to independent base dynamics, the motional basis of independent ribose as well as simultaneous ribose/base flexibility is more difficult to assess. As a first approximation to the actual motions, a simple 'Wobble-in-a-cone' model originating in the phosphodiester backbone has been assumed in these cases. Due to the proximity of the base and the C1 ,H1 vector, independent ribose flexibility cannot be due to internal ribose dynamics (Figure 22). Upon ribose repuckering from a C2 to a C3.-eo conformation, the internal ribose rearrangement causes C2.-H2, and CH while the CH-vector 3 motions, is not affected. -4- 10 C2 .-endo C3 .-endo Figure 22:Rikbe pu&aigfian C2'-to C3 erk mtinm doesnotdangethe daew oto and thenudecze. f the C -Hi waor If both moieties are flexible, it has to be considered that the underlying motions can either be concerted or independent or partly concerted (Figure23A-CQ. This uncertainty arises from the varying sensitivity of the GH vectors in the base and the ribose to different dynamic processes, depending on the nature, e. g. the direction, of the underlying motion. 124 Chapter 3: RNA Tetraloop Dynamics A B C 2s S2=S2 =S2 2 2 2 2 I Figtr 23: G V1V1/ 1 S1 a (4, m uak (B)an pany 9 W/4 oN6 2* 21 2 S2 =S2lSl, 2 S4 I -' I td nmrfor thease atSI > s2 (0 of tomra pawde 1 and2. Since the extent of motional concertedness cannot be assessed from the data, the two dynamic extremes, completely concerted motion (Figure 23A) and independent motion (Figure 23B) have been determined in here. In cases, in which both moieties are flexible and base mobility exceeds the mobility of the ribose (S2ibose>S2e, Figure 23Q, excess base dynamics have been fit with the GAFmodel. An additional simplification has been introduced for moieties exhibiting two fast time-scale motions, for which accordinglytwo order parameters (S 2 and Sj ) are available.In these cases, both the spatial restriction for the overall order parameter and the two order parameters separately has been given. However, if the moiety in question was a ribose connected to a flexible base, only the overall motional restriction (obtained from S2)has been propagated into the base in order to simplify the analysis. The results of the motional analysis of the 13C relaxation data are summarized in Table 13 and Table 13 for the acUUCGgu loop and in Table 14 and Table 15 for the auCACGgu loop at the two temperatures. In addition, the approximate base pair strengths extracted from the imino proton linewidth are given. Finally, the ribose pucker rigidity as obtained from 3 J(H1 .,H2 ) coupling constants is also listed in Table 12 to Table 15. Base pair strength as well as ribose puckering are divided semiquantitatively into different categories ranging from (+++) to (-) following the criteria described in detail in the caption of Table 12. 125 Chapter 3: RNA Tetraloop Dynamics 298K S3 S1 L1 L2 S2 Model 0 Base a pair S2 Model Ribose ox .. S2 S4 0.88 0.88 0.87 0.87 0.67 0.84 0.83 0.89 0.89 GAF GAF WGAF GAF GAF GA GAF GAF - - - 24 25o0~~ 140 Rex Base L4 GAF - o, L3 indep. conc. . . +++- - 220 . . 150 . 0.83 - 0.84 - 0.77 W 0.73 W - - ° - 150 ++ - - 0.82 - 100 . + +4 - 240 230 ... ° - 120 70 - - ++ +++ +++ 0.82 0.80 - 0.81 - Re, Pucker +++ +++ ++ ++ +++ +++ +++ Table 12 Dynanic infomution on the acUUCGgu loopat 298K The basepair strengthhas en assessed firm thepeak heightof the iino proton resonances.The basepair smrgts are categorized asfdlaos: (+++) indicatesan imino resonanceiamitie equal to the one of stable stem ridue; (++) is apliedfor only slightly deased resonances is labied am a residueis labed (+) f the rsonanceis st ngydsed but sible,(-) is appliedin the absencef a imino resonane The rigidity f the ribosepuker has been obtainedfrom the size f the 3J(H ,H2) apling 1 wanstants.(+++) is appliedforJ-crtplingslargerthan 10Hz and smller than 1Hz; (++) indiates a J-catplingof 8 to 10Hz or 1 to 3Hz; midues,for hich not tplingcotant acol aqui are indicatedbya (-). 317K ----- -- - -)4 S3 S2 S1i 0.82 0.82 0.80 0.82 Model GAF GAF GM - - - 230° , 00 Base x160 Bae Rex Base ase pair S2 Ribose Model 0 a,, Re L2 0.77 0.75 0.81 0.83 GM GAF GAF GAF 300 20 ° 19 ° 170 130 - - 190 lops 2.2s + 0.83 0.84 0.85 - ~ S4 GAF - ++ S2 0.75 ' +++ L4 GM,W 130 180 L3 indep. 0.58 ° - . - 1.5s'' ' .+ ++ +++ _______ - 0.77 0.75 0.81 0.81 0.82 W 230 W 250 - - - - - - - - - +++ 2.74s' - - .. - - Rex . Pucker L1 -conc. - .. +++ . . +++ +++ +++ Table 13: Dymnic ifrontion an the acUUCGgu loo at 317K The basepair strengthbas beenassesedfrom the peak height f the inino proton resonanes; The rigidty f the riose pudeker hs een btainedl from the seize f the 3J(H1,H2) acling cwtants. 126 Chapter 3: RNA Tetraloop Dynamics 298K S2 2 S S2 Model Base ----- ---- --+ ------ -- -- S3 0o Orx S1 0.87 0.84 Pair S z 0.83 GAF GAF GAF - 110 130 l Base L1 L3 L4 S2 S4 0.51 0.81 0.93 0.87 0.83 0.63 - - 0.82 - - - GAFW GAF GAF GAF GAF GAF 350 - 190 15° 130 120 - - - __ 0.93 (250/160) 607ps -. 0.92 S2 s2 Model Ribose 00 ax - - - - - - +++ Table 14: Dymnic ionntimn height f the imino pron 0.96 0.86 0.89 0.67 - - - - 0.82 - - - 972ps +++ + + 0.87 2 350 0 ....... ++ 0.55 W 4, Pucker idep.. 310 90 x q---++ 0.9 170 L2 conc. 0.93 ++ - . - - - - - ] ++ +++ on the auCA CGgu loopat 298K The basepair strnth hzs beenassessedfitnmthe peak oresn s; The rigdity f the rike pudeer has auplingaotants 127 n ochtaimrd firvmn the seize of thedx 3J(H1,H2) Chapter 3: RNA Tetraloop Dynamics S3 317K 317K _ conc. indep. 0.60 0.46 SI 0.80 2Sf~~~ GAF GAF GA 250 - - ';,''' o; ~, 26 ° R,~sex ."c,,~_:_ 34 ° ______ 140 I : :07 O0475' :'0, '0 0.58_ ~ S4 0.53 0.80 0.71 0.81 . - 0.73 GA GA - - 350 ' 'o - S2 __"_ GAP' 200 *' 330 3180 GA GA -- 30° o'""o 210 14 -' .7 -7.---++ ----++ --_ _Ad 6.4s~ ++ 0.77 (27/6,).-. 750ps '.i:. l7ps ...:'-:{.:..[:.: , . ',:__... . 14....~mOr . _ _ ________~~~~~~ Base Pair S2 ' 01:76- L3 L2 cnc. W,GAF e BaseBase ax : ' :'L'..-.' 2 -:: Model 1L - 0.88 . ... .1 i '..r .. .........................: '....Or 085 . .... l . .. .:6 :''.. : -: . ..... ' .. - -.... . -. 0.79 '' ...... ..... 087 14 1843ps++ (190/210) + - - 0.80 0.82 Ribose $2 Model 0e a1 0.94 W 250 ' Pucker~~~~~~~~~~~~~~~~~~ . cntut. " -. ''[ .i' - '." . 619ps R.. Pucker ' 0.84 W '" cnet : . :. ' : : i' .. :: - " ' 3.6s-- -- - +"+ .:. +. : Table 15: Dymni ifanm onon the auCA CGgu ko at 317K The basepir shth hz beenassessedfrmnthe peak heightof the im prton rarr; The igidity of the ribse pucker hs I-an adiedfin the seize of e 3J(H, H2) cokql1zngcmtanl. From this combined information, the detailed motional pictures of the two tetraloop motifs presented in Figure 24 have been constructed. In here, concerted motions have been assumed. The dynamics at 298K, at which both tetraloops are stable, can be viewed as the ground state dynamics. Since the cUUCGg and the uCACGg motif exhibit almost identical structural features, it is not surprising that their general ground state dynamic characteristics are similar. At a closer look, however, the extensive analysis conducted in here allows for the identification of quantitative differences in loop dynamics. The most pronounced difference can be found in residue L2. While in the uCAGGg loop the whole nucleotide exhibits fast internal motions, the flexibility of residue L2 in the cUUCGg loop is smaller in its base and even smaller in its ribose moiety. In addition, the other residues show slightly different dynamics in the two loops. Residue L3 is more mobile in the ribose moiety than in the base in the cUUCGGgmotif, while it exhibits a rigid behavior in the uCACGg motif. 128 ,. . Chapter 3: RNA Tetraloop Dynamics cUUCGg 298K 5' 5' 317K 3' uCACGg ,, - L2 S1 S3 5 298K 3' 5' Figur 24: Dynis 317K 3' f the cUUCGg(top)and the uCA CGg (boawo loop at 298K (left) arrnd317K (night). The oazerall dynaznis based on S2 are gizn For nvt, zhrichpossessa 2 term d errtom 1, -r is gizen 7he 'Wobbir-a-re' nmel s depitad as mm, te GAF-rm ei as duradararnro. 129 Chapter 3: RNA Tetraloop Dynamics Residue L4 is remarkable in that it represents one of the most stable residues overall in the uCACGg loop at room temperature but has a slightly flexible base in the cUUCGg loop with a ribose moiety of average stability. Imino proton line widths are in agreement with the ground state dynamics in that the L1:L4 loop base pair and the two adjacent stem base pairs are intact. In case of the cUUCGg loop, the increased mobility of riboses L2 and L3 in absence of ribose repuckering points to increased flexibility of the entire phosphodiester backbone in the upper loop region. At 317K, close to the melting temperature of the uCACGg motif, the relative dynamics of the actual loop residues do not change for both motifs except for the slightly increased flexibility of the base at position L4 in the uCAGGg loop. From this, it appears that all of the secondary structure features of the cUUCGg and most of the uCACGg loop can still be present at 317K. Thus the backbone interaction of the L3 base and the extensive base stacking of residues S1, L1 and L3 remain unperturbed (Figure 24). While the dynamics of the loops are thus more or less temperature independent, the two base pairs adjacent to it exhibit increased dynamics in the uCACGg loop, while the stem of the cUUCGg motif remains unperturbed. At higher temperature, the two purine bases of the base pairs adjacent to the uCACGg loop become about as flexible as the non-interacting residue at L2, while neither of their respective base pairing partners show increased flexibility. Although one of the two base pairing partners exhibits increased dynamics, in both cases, the hydrogen bonding arrangement remains at least partially intact as apparent from the imino proton line width analysis. In contrast, although L4 exhibits only a minor increase in flexibility and the flexibility of L1 does also not change significantly, the imino resonance of L4 has vanished completely at 317K. Thus, while the strong increase in flexibility at positions S2 and S3 does not result in a complete disruption of the base pair arrangement, the hydrogen bonds of L1i:L4 is broken without a significant increase in local dynamics. The imino resonance of L4, however, reports only on the two base-to-base hydrogen bonds in the L1:L4 base pair. The third hydrogen bond between the L4(0 6 ) and the ribose 02' of L1 can not be monitored and could thus still be present. Furthermore, additional means of stabilization like base stacking could keep the uCACGg loop structure intact. 130 Chapter 3: RNA Tetraloop Dynamics 3.4 DISCUSSION In this work it has been attempted for the first time to characterize RNA dynamics in a way that every residue is considered both in its ribose and in its base moiety. The approach was to measure NMR autocorrelated relaxation parameters of C1, in the ribose and of C6 or C8 in the base moiety, translate them into motional parameters by a common model-free analysisand interpret them further by application of appropriate motional models. The aims were to (i) investigate the validity of the model-free approach for 13Crelaxation data in RNA. (i) scrutinize the relevance of the motional parameters obtained from the model-free analysis in order to understand the determinants of stability as well as flexibility in a biologically relevant system. The dynamic investigation has been focused on the abundant RNA tetraloop family of the sequence YNMG. Two members of this family, the exceptionally stable cUUCGg motif and the uCACGg motif, which exhibits a similar fold but decreased stability, have been studied. In order to determine the origin for the different loop stabilities on a molecular level, dynamic investigation was carried out both at room temperature and around the melting temperature of the uCACGg motif. The results of the dynamic analysis are discussed in the following both in regard to general technical aspects as well as to the specific biological implications. 3.4.2 Model-free analysis Application of the model-free formalism to a nucleus requires on the one hand isolated I-S spin system type behavior and on the other hand knowledgeabout its CSA. While the model-free formalism has been developed for isolated I-S spin systems, it has been applied herein to study the dynamics of nuclei (C,, C6 and CQ)with not only a directly bound proton but also an additional adjacent carbon spin (C2 , and C5 ). In agreement with earlier studies on small DNA molecules [38, 39], it has been shown in here that the additional dipolar relaxation contribution can be neglected for the size of the investigated molecules (Figure 14). Even for the larger of the two molecules,the 30-nt RNA, the relative CCdipolar contribution amounts only to about 1%. 131 Chapter 3: RNA Tetraloop Dynamics It could be shown here that in contrast to the neglectable CCdipolar contribution the CSA constitutes a more crucial factor in the interpretation of 13C relaxation rates (Figure 13). Especially for the aromatic C6 and C8 , which possess large CSA values, knowledge about the size of the CSA is of essential importance in order to interpret relaxation parameters. There are two studies on carbon CSA values in nucleic acids available to date [25, 26]. From the analysis of the relaxation data it resulted that it was in agreement with similar CSA values for C6 in both pyrimidines and for C in both purines as reported in ref. [25]. Consequently, the 13C relaxation study constitutes a measure to assess the validity of these more or less theoretical tensor values for their application under physiological conditions. In addition to the absolute value of the CSA, also the orientation of the CS-tensor is relevant in the case of anisotropic molecular diffusion. As demonstrated in here, for RNA, an axially symmetric diffusion tensor has to be applied already for molecules as small as the 14-nt RNA in order to grant accurate dynamic interpretation of the dynamic data (Figure 16). While in the model-free analysis an axially symmetric CS-tensor with the unique main component oriented along the I-S internuclear vector is assumed, all 13 C tensors in nucleotides have been reported to be fully anisotropic with their principal axis tilted away from the CGHvector. From the present analysis, the incorporated CSA values as well as the assumption of an I-S spin system type behavior have been validated by the similarity of both the axially symmetric diffusion tensor and the overall correlation time ;c obtained from the model-free analysis and the hydrodynamic calculations as well as the ability to fit most of the relaxation data satisfyingly. In addition, for both investigated molecules the stably base paired stem residues exhibit very uniform dynamics as expected. Furthermore, at temperatures, at which both loop motifs are stable, their dynamic profile is in agreement with their structural features. In spite of these in general reassuring results, systematic deviations for the cytosine base dynamics have been noted, which are most likely due to deviations of the actual CS-tensor from the applied one. Model-free analyses of RNA will become more precise, if at the one hand CS-tensors of RNA carbon spins are determined in more physiological systems such as directly on oligonucleotides in solution. In principle, the CS-tensor can be determined from the geometric information conveyed in multiple cross-correlated relaxation rates correlating the CS-tensor to the different neighboring dipole-dipole vectors or from the anisotropic chemical shift information extracted from samples in different alignment media. For proteins, a number of studies have been carried out along these lines 132 I......__ Chapter 3: RNA Tetraloop Dynamics aiming at the determination of the amide 15 N CS-tensor in solution [60-62], which could be transferred to carbon spins in RNA. For both the imino nitrogens and various carbon spins, S2 parameters have been determined in earlier reports. From the 13Crelaxation rate analysis of the 14-nt RNA presented in here, averaged S2 stem values of 0.88 +0.003 and 0.81 +0.006 have been obtained for the base moieties at 298K and 317K, respectively. For the ribose, stem S2 parameters of 0.83_+0.001 and 0.87+0.001 have been determined at 298K and 317K, respectively. A 1 5N relaxation analysis has been conducted on the 14-nt RNA studied here [59], reporting S2 values for the base paired guanosine and uridine residues (G1, G2, U6, G9, G10, Ul 1 and G12). The S2 values obtained in the in the 3C 1 5N relaxation data analysis are compared to the ones acquired for the bases analysis in Figure 25. Apart from G9, the order parameters in the 1 5N study are significantly lower (0.74 to 0.81) than the ones determined in here. Thus, the average S2 value of the stem residues amounts to only 0.78 +0.01. While G9 seems to be the most stable residue according to the previous report, it appears even slightly less stable than the stem residues in the "3C relaxation data analysis. In addition, the relative stability of G10, U1l and G12 is reversed. 1 - 0.8 N cn stem 0.6 nfAvt/i Wl loop G G C A I I 1 2 CU > stem U C G G U G I I I I I I 3 4 5 6 7 8 I I I I 9 1011121 C C I I 314 Residue Figwre25:S2uluesfinth 'C dandataaalysz (Haae)at 298Kandfr '1N axaiodata(rey)potid in ref [59. 133 Chapter 3: RNA Tetraloop Dynamics It has to be noted that the 15N analysis was carried out at 273K, while the 3C data have been obtained at 298K. Considering the differences in temperature, it is even more surprising that the l5 N analysis reports higher flexibility. As for 13C also ' 5N relaxation data analysis relies on knowledge about the CSA. Thus, the respective CSA-values could be underestimated in our or overestimated in the 15 N relaxation report. Apart from that, it is possible that due to the different orientation of the N-H as compared to the GH vector in the bases, "5 N and "3Crelaxation report on different motions. In contrast, other studies on 3C relaxation in different RNA molecules are more in agreement with the data presented in here. Thus, average stem S2 values of 0.8 for C2 and C8 in purine bases have been reported at 298K for the 16-nt iron responsive element RNA hairpin [37] and 0.7 to 0.9 for C6 and C in the 29-nt ATAR RNA [63], while slightly higher stem S2 values of 0.8 to 1.0 have been determined for the adenine C2 in the 30-nt TAR RNA at 298K [42]. In small double stranded DNA, averaged S2 values of 0.8 and 0.6 have been reported at 303K for the base and the ribose carbons, respectively [35] indicating an increased ribose flexibility. In contrast, an averaged order parameter of 0.8+0.09 has been reported for thymine C1 . [39] and similar order parameters (0.8+0.1) were obtained for both base and ribose carbons at 303K [32] as well as for two DNA octamers (-0.8) at 298K [34, 64]. 3.4.3 Dynamics of the YNMG tetraloop motif The starting point of this research was to understand the factors, which trigger RNA stability in as much detail as possible. Dynamic investigations by NMR relaxation data analysis seemed appropriate for this task, since they report on both the structure and the flexibility on a moiety as small as a bond vector. In a simplified model, this vector can be interpreted as a dynamic reporter for a moiety like the base or the ribose in a nucleotide. It has, however, to be pointed out that this simplification is only valid, as long as the moieties are not subjected to internal motion. While this is always true for the internally rigid base moiety, the ribose might undergo repuckering motions. In order to assert ribose pucker rigidity, 3 C relaxation data have been combined with J(H1 ,H2 .) coupling constants in here. However, even in a rigid arrangement, the relaxation data is not obtained for the whole moiety but for a given CH vector, which in turn is sensitive to a different degree to different motional events depending on their relative orientation. Therefore, the amount of flexibility extracted from relaxation data does not necessarily account for all the dynamics of a moiety. In order to improve the 134 Chapter 3: RNA Tetraloop Dynamics dynamic investigation, multiple dynamic probes should be used for a given moiety. This, however, implies lengthier data acquisition and analysis procedures and might even render the analysis more confusing, since different vectors report on different motions without provision of information on the underlying motional events. 3.4.3.1 Ground state dynamics Comparison of the cUUCGg and the uCACGg motif at room temperature reveal an overall similar but not identical dynamic picture. Despite its decreased thermostability, the uCACGg motif is not the more flexible one. Nevertheless, it contains the most mobile residue at position L2, while the remainder of the loop is rigid. In contrast, the cUUCGg motif exhibits smaller,yet more delocalized dynamics in the upper two residues (L2 and L3). These differences in the dynamics could arise from slight variations in bond lengths or in the extent of base stacking interactions due to the difference in the primary sequence. One of the questions in the study of dynamics is to which extent they are actually coupled to structure. In case of the actual loop region of both motifs studied in here, the dynamics are in complete agreement with the structure, pointing to a close structure-dynamics relation at room temperature. To what extent the differences observed between the two motifs can be attributed to deviation from the strict structure-dynamics relation or arise from slight structural differences is debatable. The effect on stability of single or multiple nucleotide replacements in the UUCG motif has been extensively studied [12]. In the present case, the exchange of a uridine for a cytosine at position L1 signifies the exchange of an oxygen for an amino group, both of which are not engaged in stabilizing interactions. In addition, the exchange of a uridine for an adenine at position L2 does not involve any change in secondary structure interactions. Thermodynamic studies have shown, however, that both nucleotide exchanges are unfavorable in regard to the thermostability, both separately and in connection with each other. The gain in stability is, however, only marginal. Thus, the melting temperature of the cUUCGg loop is 72.9°C, while the one of the uCACGg motif amounts to 69.6°G If L2 of the cUUCGg is replaced by an adenine (cUACGO), the melting temperature drops by 2°0 G Under the assumption that flexibility can be correlated with stability, the increased dynamics of an adenine at position L2 as compared to an uridine offers a first insight into the reasons for these differences in thermostability upon exchange of a base, which is free from interactions. Thermodynamic studies on different tetraloops [12] also demonstrate that the effects of nucleotide exchanges are not independent, but vary within different sequence context. Thus, while 135 Chapter 3: RNA Tetraloop Dynamics an adenine at position L2 represents the least stable choice in a CNCG loop, for an UNOG loop, the cytosine variant is the least stable one. Alternatively, the differences in loop dynamics could be also attributed to remote effects of the closing base pair. In contrast to an CG Watson-Crick base-pair, a U:G wobble base pair possesses only two hydrogen bonds and causes local differences in the helix structure [1], which could propagate into the loop and account for the observed dynamic differences. One of the attractive features of dynamic investigations is their content in both dynamic as well as structural information, which can serve to report not only on actual changes in stability but also on dynamics in an otherwise stable arrangement. This can help to identify unstable structural features within a structure even under stable conditions. From the comparative study at a temperature, at which both loops are stable, no putative later melting sites in the uCACGg motif can be identified, since the dynamics are completely congruent with the structural features. 3.4.3.2 Melting of the uCACGg motif While the dynamics of the cUUCGg motif remain more or less unaltered at higher temperature, the uCACGg motif exhibits large dynamic changes in several residues. Apart from a general gain in flexibility, the dynamic profile of the loop remains almost unperturbed at higher temperature and most of the initial stabilizing interactions are still possible. Hence, as expected, the sequence difference in the actual loop region does not constitute the deviation in stability from the cUUCGg motif. In contrast to the actual loop, one of the residues of the closing base pair and one adjacent to it acquire flexibility equal to the dynamics of the free base of position L2. The stability of the respective base pairing partners and the presence of, however, weakened hydrogen bond in the base pair point to a more or less unperturbed structure. This signifies, that at 317K the initiation of uCACGg melting is observed. From the combined data presented in here, the structural and dynamic features of the uCACGg motif at the initiation of melting given in Figure 26 have been extracted. In contrast to the situation at room temperature, at 317K, the observed dynamics deviate from the structure. While hydrogen bonds can still be observed for both the closing base pair S1:S2 and the adjacent one S3:S4, the flexibility of one base pairing partner in each base pair is highly increased. In contrast, L1 remains completely rigid and L4 gains only slightly in flexibility although no hydrogen can be observed for this base pair. Only from the dynamic information it becomes evident that the two base pairs adjacent to the loop and not L1:L4 constitute the primary melting site. 136 .. . Chapter 3: RNA Tetraloop Dynamics 7;VI ulual y - aJ ma melting site Primary melting site * % 5' 3' FiguWe26: lMdg de EuCACGglp. A nives andtm sales qfrtr amre gn rie nety oS2 (shd dakgry). No data wdd be aimd fr the Due to signal overlap, no information on the ribose moiety of S2 could be obtained. This increases the difficulties in elucidating, which of the two base pairs (S1:S2 or S3:S4) constitutes the origin of melting. Although the overall S2 values for the two flexible base moieties of resides S2 and S3 are very similar (0.53+0.06 and 0.46+0.01), they exhibit dynamics on widely different time scales. Whereas S2 shows motions on two fast time-scales (< 10lps and 1800ps), the flexibility of S3 is due to only one high amplitude, fast time-scale (< l10ps) motion. Apart from that, the imino proton line width indicates about the same strength in residual hydrogen bonding. Hence, although differences in dynamics can be detected, it is not possible to narrow the identity of the melting initiation site further down to any one of the two base-pairs adjacent to the loop, since no information on the motional bases of the observed dynamics can be obtained from the data. The slightly increased dynamics of the L4 base and the absence of the L1:L4 base:base hydrogen bonds indicate that L4 constitutes the secondary melting site, through which the stem melting is propagated into the loop. 137 Chapter 3: RNA Tetraloop Dynamics In conclusion, the dynamic investigation of the YNMG tetraloop motif presented here demonstrates that loop stability is not only triggered by the nature of the closing base pair but also depends on the one preceding it. While the significance of the closing base-pair as a determinant for loop stability has been long recognized and extensively studied [12, 19, 65], the effect of more remote base pairs has not been acknowledged so far. 3.4.3.3 Biological implications Why does the same RNA secondary structure motif appear in so widely different sequence context with such a difference in stability? Why, if a low melting temperature is required for the SLD in the Coxsackievirus, is the thermostable CAGG tetraloop not replaced by a less stable loop motif? An explanation for the necessity of an unstable member of the YNMG motif at this position on the viral genome could arise from the different requirements in this sequence. On the one hand, the recognition of SLD bythe viral precursor protein 3CD P° is purely structure based [1]. Thus, protease binding affinity remains unaffected, when the tetraloop is replaced by a UGCG motif [1]. On the other hand, the secondary structure of SLD has to melt in order for the replication of the viral genome to take place. It follows that while SLD has to be highly structured for protein-recognition, the increased stability accompanying the structural content is not favorable for the low stability required for replication (Figure 27). In addition, none of the loop residues is especially conserved [20], the most conserved being the Gsy at position L4 (85%), followed by position L3 (73% ). The A at position 2 occurs only in 52%, while the most frequent nucleotide at position L1 is, U, is conserved only in 48% of the sequences (C is found in 27%). In contrast, the G of the closing (97%) base pair and the two adjacent base pairs (90% and 100%) are highly conserved. The conserved stem-residues contain also the residues, which acquire increased mobility at higher temperature, implying that the decreased stability of the closing- and the adjacent A:U base pairs is biologically relevant. It is possible that the stem melting is relevant for initiation in viral RNA translation. Apart from the recognition by the 3CDP ° protein, the YNMG motif at this position might be required for reliable folding of the highly structured 5'-non-translated region of the viral genome. 138 . . Chapter 3: RNA Tetraloop Dynamics A B 5' Figure 27: Tfd 3' - 5' 3' dernnd onSLD. Suaal stabilityisnrtdnfor bin or3C (4); sm for stsraraxpdwi g eplicaionofdx Hralram (B). ralcfiexibiltys m d 3.5 OUTLOOK This study has for the first time presented an almost complete dynamic picture of an abundant RNA secondary structure motif. Comparativestudies of the cUUCGg and the uCACGg motif of the YNMG tetraloop family demonstrate that loop stability is triggered not only by the nature of the closing base-pair but also by the identity of more remote base-pairs at least one position away from the loop. This stability fine-tuning seems to be used by nature to decouple structural and stability requirements in order to adapt hairpin structures for opposing purposes. The study presented constitutes the first step in investigating the effects of remote base pairs on loop thermodynamics. In the future, systematic studies to this purpose should follow. 139 Chapter 3: RNA Tetraloop Dynamics 3.6 REFERENCES 1. Ohlenschlager, 0.; Wohnert, J.; Bucci, E.; Seitz, S.; Hafner, S.; Ramachandran, R; Zell, R.; Gorlach, M. (2004). The Structure of the Stemloop D Subdomain of Coxsackievirus B3 ue (Cam), 12, 237-248. Cloverleaf RNA and Its Interaction with the Proteinase 3G S 2. Noller, H. F. (1984). Structure of ribosomal RNA. A 3. Tuerk, C; Gauss, P.; Thermes, C; Groebe, D. R.; Gayle, M.; Guild, N.; Stormo, G.; d'Aubenton-Carafa, Y.; Uhlenbeck, O. G; Tinoco, I., Jr.;et al. (1988). 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Yamazaki, T.; Muhandiram, R; Kay, L. E. (1994). NMR Experiments for the Measurement of Carbon Relaxation Properties in Highly Enriched, Uniformly 13C, 5 N-Labeled Proteins: Application to 3QCCarbons. JAm ClemSoc, 116, 8266-8278. 59. Aklike,M.; Fiala, R.; Jiang, F.; Patel, D.; Palmer, A. G., 3rd (1997). Base dynamics in a UUCG tetraloop RNA hairpin characterized by 5N spin relaxation: correlations with structure and stability. RNA, 3, 702-709. 60. Tjandra, N.; Szabo, A.; Bax, A. (1996). Protein Backbone Dynamics and 5N Chemical Shift Anisotropy from Quantitative Measurement of Relaxation Interference Effects. J Am Chan Soc, 118, 6986-6991. 61. Fushman, D. and Cowbumrn,D. (1998). Model-Independnet Analysis of '5 N Chemical Shift Anisotropy from NMR Relaxation Data. Ubiquitin as a Test Example. J A m em Soc, 120, 7109-7110. 62. Boyd, J. and Redfield, C (1999). 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NMR-investigation of the T-cell receptor 4-chain in solution and bound to lipid micelles. 145 Chapter 4: Structure of the TCR C-chain Specific Aims The goal of this research was to contribute structural information from NMR experiments to a functional investigation of the early events of T-cell activation upon antigen interaction. The investigation was focused on the cytoplasmic portion of the T-cell receptor (TCR), its C-chain, the putative mediator between the extracellular antigen and the intracellular signal transduction cascade leading to T-cell activation. Earlier studies resulted in a T-cell activation mechanism that proposed a TCR state dependent lipid incorporation propensity of the -chain accompanied by a folding transition [1]. In order to support this proposed mechanism, standard protein NMR assignment and secondary structure elucidation techniques have been applied to TCR g bound to detergent micelles in order to obtain the structural characteristics of this folding transition in a residue resolved manner. In addition, the assignment of free TCR 4 constitutes the basis for residue specific investigations on its interaction with the HI-V-proteinNef, the interaction of which with TCR ~ has been shown to impair T-cell function through a number of different mechanisms [2-4]. In addition the recently reported dimerization of TCR 4 [5] has been investigated. TABLE OF CONTENTS 4.1 INTRODUCTION 4.1.2 4.1.2 4.1.3 4.1.4 4.2 4.2.2 4.2.3 4.2.4 4.2.5 4.2.6 4.2.7 4.3 ................................................................................................. 148 148 T-Cell Activation ................................................................................................................ 149 The TCR -chain ............................................................................................................... TCR /Nef interaction....................................................................................................150 Protein backbone resonance assignment........................................................................152 MATERIALS AND METHODS ............................................................................ 154 154 Protein expression.............................................................................................................. 154 Backbone assignment of free TCR ............................................................................... Concentration dependent experiments ...........................................................................155 Temperature dependent experiments ..............................................................................155 155 ~/Nef interaction studies .................................................................................................. 156 TCR in LMPG micelles.................................................................................................. RESULTS ................................................................................................................ 157 157 4.3.2 TCR in solution............................................................................................................... 157 4.3.2.1 Backbone Assignment ................................................................................................... 162 4/Nef-interaction ........................................................................................................... 4.3.2.2 146 Chapter 4: Structure of the TCR ;-chain 4.3.2.3 /~-Dim erization ............................................................................................................ 166 4.3.3 TCR 4 bound to LM PG-niicelles ..................................................................................... 169 4.4 CONCLUSIONS ..................................................................................................... 174 4.5 REFERENCES ....................................................................................................... 176 147 Chapter4: Structure of the TCR C-chain 4.1 INTRODUCTION 4.1.2 T-Cell Activation T-cell activation is initiated by binding of its surface located T-cell receptor to antigens presented by major-histocompatibility complex (MIC) proteins on the surface of body-cells. This process involves the interaction of several associated proteins on either cell surface (Figure 1). nntiaen nresentinacell TC Tcell .,"- U Figur 1:T-d mweptorantintml c. Antigen binding is followed by TCR clustering [6, 7]. This leads to multiple phosphorylations of the TCR C-chain cytoplasmic domain at specific so-called ITAM sequences gmmunoreceptor Tyrosine- based Activation Motifs) by the tyrosine-kinase Lck and/or other members of the tyrosine-kinase family [8-10]. Phosphorylation of TCR ( constitutes the starting point of the intercellularsignaling cascade resulting in T-cell activation. After phosphorylation TCR ~ binds to and activates the cytoplasmic tyrosine kinase ZAP-70 (or Syk) through interaction with its tandem SH2 domains [11]. Bound ZAP-70 then activates other tyrosine and serine-threonine kinases, induces phosphatidyl inositol turnover and binding of adapter molecules as well as other processes in the early phase of Tcell activation [12, 13]. 148 Chapter 4: Structure of the TCR 4-chain 4.1.2 The TCR 4-chain The invariant C-chain of the T-cell receptor is a 164 amino acid single-pass transmembrane protein, which exists as a disulfide-linked homodimer within the receptor. Its Gterminal cytoplasmic domain of 112 amino acids carries three ITAM motifs of the consensus sequence Yxx(L/I)x, 8 Yxx(L/I), where x can be any amino acid (Figure 2). During T-cell activation, the ITAM motifs are phosphorylated to a varying degree at different tyrosine residues. ; ITAM1 GSIRVKFSRSADAPAYQQGQ NQ. LI 'L//DKRRGRDPEMGGKPRRKNPQEG 10 20 30 ITAM2 tQKDKKQA 70 40 50 60 ITAM3 GMKGERRRGKGHDGL|STZlTKDHMQALPPR 80 90 100 110 Figure 2: Pirwy some ef x 7TCR -chinOtpinic damn asit hasbLenstudid Ther7x e s canies m an acds of its tramnwraw dmin at its N-tiu. 1Thx dshed wd1 ln nwks he gmg ce tclasrnic doami Thet ITAMseques amre rimt ndark grey(YxxL-rr andligtg y( eiablienkersoxts). Tyrsit msduhi, can ateidng Tcd acti , arshan l&tgy The mechanism, by which TCR clustering is linked to intracellular C-chain phosphorylation, is not yet well understood. Unlike other receptors activated by clustering, TCR g does not possess any intrinsic enzymatic activity or associated kinases, nor do the TCR antigen binding domains appear to undergo any significant ligand-dependent conformational changes, which could account for signal mediation across the membrane. Amongst the various mechanisms proposed for signal transfer are: subtle conformational changes below the resolution of the available crystal structure [14], allosteric changes in the TCR due to ligation [15], co-localization of co-receptor-bound kinases with their substrates on TCR cytoplasmic domains (as both bind to MHC proteins) [16] and large scale reorganizations of membrane proteins [17]. Recently, it was found by the group of Prof. Stem that the intrinsicallyunstructured TCR 4-chain undergoes a structural transition to a more a-helical state upon interaction with acidic lipids [1]. This lipid induced folding transition as well as the immunity of TCR ~ to phosphorylation by intracellular kinases in its lipid bound state, has led to the proposal of the signal transduction mechanism presented in Figure 3. In this model, TCR ; is embedded in the membrane with its ITAM sequences sequestered away from any cytoplasmic kinase in the resting T-cell. Upon binding of antigen loaded 149 Chapter 4: Structure of the TCR -chain MHCQ,TCR clustering results in a steric release of the 4-chain from the membrane and thus renders it amenable to phosphorylation. This T-cell activation model has been the outset of a collaboration between our group and the one of Prof. Stem aimed at the structure determination of the 4-chain cytoplasmic domain in its lipid bound state by NMR. The objective of the project was to investigate whether the structure of LMPG- bound ~ provides an explanation for the impossibilityto phosphorylate this species. Resting State Receptor Clustering Activated State Immune Response Figume3: Ped Structure adoption of TCR sigrp tranrsdmin rdmsm for Tell aition mniatd by TCR 4 upon micelle-interaction was probed by a chemical shift index (CSI) study of the HA chemical shift changes. As described in the introduction, the a CSI is sensitive to ac-helical and -sheet deviations structure deviations from the random coil. 4.1.3 TCR /Nef interaction Nef (negative factor) is an accessory protein found in human immunodeficiency virus (HIV) type 1 and type 2 as well as in simian immunodeficiency virus (SIV). Although it does not possess any 150 Chapter4: Structure of the TCR 4-chain intrinsic enzymatic function and is not required for virus replication, it is mandatory for achieving and maintaining high viral loads in ziw [18]. It does so by interacting with various cellular signaling pathway as well as immune cell specific proteins. One of its effects is a reduction in the number of CD4 receptors on the surface of infected cells by binding to the cytoplasmic domains of CD4 [19]. CD4 receptors play a role in preventing reinfection by budding virions. Stimulation of the viral replication has been linked to the interaction of Nef with the SH3 domain of Src family tyrosine kinases [20-23] as well as a serine/threonine of Nef to TCR C kinase [24-26] and protein kinase C theta [27]. Binding has various different effects: It has been connected to upregulation of the so called Fas-Fas ligand interactions, which lead to apoptosis [4]. In addition, interaction between Nef and 4 results in the downmodulation of the complex formed by the TCR and CD3 and thereby reduces the availability of CD3 for stimulation by cross linking with anti CD3s antibodies [2]. By means of multiple deletion mutants, two independent Nef binding sites have been identified within the cytoplasmic domain of TCR ~, each of which overlaps with an ITAM sequence (Figure 4) [3]. Transmembrane Domaine N o Cytoplasmic Domaine ft -ITAM 1 ITAM 2 ITAM 3 \ 3 24 34 _ 74 //?79 * Figure 4: TCR /Ne f Sveraawnsites as detemi by ddain and mdte alnm sutm interaazn sies ardual ae shon ekI Residuesdt am dal for Nef burig sed n nragsi aremhigbiMi The ricke,wibm of the ytqolasnicdonflow the wmlae m For this study, only the FC 115 rrnagembis [3]. The aim s', d in the nerf the 120 amino acid core domain of the -27 kDa SIV Nef has been used, since the full length protein tended to aggregate at higher concentrations. Simian Nef was used instead of the HIV Nef because of better expression yields.A binding constant of -0.3 to 2 ILMof SIV Nef to TCR ~ has been determined by surface plasmon resonance by our co-workers. In order to characterize the binding site of Nef to TCR 4 by NMR, H and 15N chemical shift perturbation studies upon addition of Nef to TCR ~ were carried out. This required the backbone resonances assignment of the free C-chain, which as well as the one of the lipid bound form was obtained from standard protein assignment experiments. 151 Chapter4: Structure of the TCR C-chain 4.1.4 Protein backbone resonance assignment Protein resonances assignment starts with and is often limited to the assignment of the backbone H, C, HIF, N and C resonances within each residue. The assignment strategy for a known amino acid chain follows two basic principles, connectivity and resonance pattern specificity. Connectivity between residues can be established by exploitation of interresidual through bond (scalar couplings) or through space (nOe) interactions. In addition to resonance connectivity, a varying degree of residue type information is conveyed in these experiments depending on the uniqueness of the resonance pattern. Obviously the extent of amino acid type specific information decreases with the distance from the side chain from dC and C to N and C. While residue specific information is vital to pin assignments to the amino acid sequence, it causes resonance overlap for stretches of identical or chemically similar residues. In order to achieve optimal assignment, purely sequential experiments are complemented with those conveying sequential as well as residue specific information and exclusively residue specific experiments. In this report, among the variety of available NMR assignment experiments, 3D-HNCOCO or 3D-HNCACO spectra were recorded for purely sequential assignment, 3D-HNCACB spectra complemented the sequential assignment as well as provided residue type specific information and 3D-HCCC)NH information. spectra yielded residue type specific The correlation pathways and the resulting spectra of these NMR assignment experiments are depicted in Figure 5. The nomenclature of the experiments reflects the underlying magnetization transfer. The underlined nuclei are the ones, which chemical shift is evolved within the experiment. 152 Chapter 4: Structure of the TCR c-chain HNCACO R R I I I IC 55 C 1 13 //-N- CC' IN H 11 8 R ~~~~~~~~~~~I C'--C- 55C C'- NIa H i-1 C'-// CI . .. IN ... 1+1 i : i-1 : i-2 N Hi-1 HNCOCO R R R I I I C1 4 C i+1 4C R. A & .............. .... I 1I-N- Ca-C C'N-CaN- C'-N NC- C-1 15 H HN i-1 "lI C ... i. ! 15 .... ..i.. . . i-2 i-1 i+1 i _ . N Hi-l HNCACB R R R I I I 35 C //- N 35 Ca- ...--- HiN c-- *C'-N *Ca~ C -// IN1 HN H i-1 i+1 i HCCCONH H R H Ce HNH55 0 R I I Cj 15 I//-N- C- C'-N!i-1 R Ca- C'- H i-! N- C- C'--// iN H il- i N Figure 5: Rernt armus; bken arrm NMR hkdeb sigrf transfer H1 assignmnt epennt. N lHi Resonane transfer by scalar aplings is iicated by slid thrgh strong mopling by TOCSY rrxing squers. The mopling camtants for the transferavregewn in gy The spins detea in the pexnt are underlinedin the e xn t narm and iicated by uhite baes. The resonanepattens zeithinthe HN-C or HN-H aliphaticplanesare shozensdemzticaJlyfor the adaent ridues i and i-1for ehx exnnent Hal' in thebhottonpad sigrif thealiphaticside-dhain hb)drgr. 153 Chapter 4: Structure of the TCR ~-chain 4.2 MATERIALS AND METHODS 4.2.2 Protein expression The whole protein expression and purification procedure was carried out by A. Sigalov in the laboratory of our collaborator Prof. Stem. 15N- as well as "5N, 3C labeled cytoplasmic domain of TCR g of the sequence shown in Figure 2 was expressed following the protocol given in ref. [5]. The core domain (residues 92 to 236) of SIV Nef was also expressed in Prof. Stems laboratory. 4.2.3 Backbone assignment of free TCR C The backbone assignment of the free TCR ~ in solution has been carried out using a fully 3C, 5 N labeled 1mM sample in 20mM phosphate buffer at pH 6 and 278K and 310K. In order to improve the resolution in the 5N dimension, semi-constant time versions of standard 3D-HNCACB [28], 3D-HNGOCO and 3D-HCCCONH [29] NMR experiments were carried out on 600 MHz Bruker spectrometers equipped with a IH,{ 3 C/ 15N}-triple resonance probe or a H,{13 C/15 N}-triple resonance cryoprobe. The experimental conditions are summarized in Table 1. In all experiments, C and C coupling to nitrogen was removed by application of selective refocusing pulses (G3.256, 5001xs)centered at 38 ppm and 174 ppm in the nitrogen evolution period. Side chain protons were decoupled from carbons by the same pulse centered at 38 ppmr. CC TOCSY transfer was achieved by application of a WALTZ sequence of 97ms using a 90{s carbon pulse. The experiments have been processed using Bruker xwinnmr software. The resonances assignment has been carried out in the program xeasy. 'H chemical shifts were referenced directly to 3-trimethylsilyl propionic-2,2,3,3-d 4 acid sodium salt (MSP). 13C and ' 5N chemical shift referencing was deduced indirectly from the H referencing. F1 Nuc TD T F3 F2 SW OFF Nuc TD SW OFF Nuc TD SW T OFF [K] 310 278 16 16 HNCACB 1H 1024 13C 110 60 41 15N 64 21 118 1H 1024 9 9 4.7 HNCACB HNCOCO 4.7 13C 15N 48 20 4.7 4.7 13C 174 15N 28 19.6 310 8 1H 11 11 117.2 117 HNCOCO 1024 1024 60 11 40 1H 62 90 5.5 174 1sN 64 21.1 118 278 8 HINCOCO) 'H 1024 11 4.7 13C 5.5 174 15N 64 21.1 118 310 8 HCCGONH 1H 1024 4.7 1H 100 100 128 8.5 4.7 15N 64 22.5 118 310 4 Table 1: Badeb j8.5 13C pnts 7Th 4. T he detect mdeus (Nut), the mirr refnlec e faiemr y (OFF) inppmfir & dinrm onef h epetinrnt ae gen assigmrentexpermnr for fie (iD) and the spearaluiah (SW) and dx thogd"r w dx nwir jtramww ae refr z& vvnm (NS). 154 Chapter4: Structure of the TCR ~-chain 4.2.4 Concentration dependent experiments 'H," 5 N-HSQC spectra with concentrations of 0.4mrnMand 0.01mM "5 N-labeled TCR 20mM phosphate buffer at pH 6 were obtained in subsequence to each other on a Bruker 600MHiz spectrometer equipped with a 1 {C/ 5 N} cryoprobe at 278K. For both experiments the proton and the nitrogen offset was set to 4.69ppm and 118pprm,respectively. 62 complex points were acquired in the nitrogen dimension with a spectral width of 21ppm. 16 transients were obtained for each increment in the indirect dimension for 0.4 mM sample, while 786 transients were used for the 0.01mM sample. 4.2.5 Temperature dependent experiments In order to transfer the assignment of free TCR ~ from 278K to 310K, 1 H,N-HSQC spectra were obtained out in steps of 10 C or 2°C depending on signal overlap. The spectra were recorded on the 13CQ 5N-labeled 1mM of TCR 4 sample used in the backbone assignment experiments on a Bruker 600 MHz spectrometer with a 3 C/ 5 N} probe. LH,{ The 5 N-offset was set to 117.5ppm, 256 complex points were acquired with a spectral width of 23ppm in the ' 5N-dimension. In order to suppress resonances splittings due to carbon-nitrogen scalar couplings in the indirect dimension within the doubly labeled sample, selective carbon pulses (G3.256, 250,us) were applied in the nitrogen evolution period on C. (38ppmrn, on resonance) and C (offset of 21000Hz from the carbon carrier frequency). 4 transients for each increment in the indirect dimension were applied for spectra between 278K and 283K and 8 for spectra between 285K and 310K 4.2.6 /Nef interaction studies In order to study binding dependent chemical shift perturbations, H,1 5N-HSQC spectra were recorded at 298K for free 5N labeled 4 and 15N labeled g in the presence of a twofold excess of unlabeled SIV Nef core domain. Measurements were carried out in 10mM phosphate buffer in the presence 100mM NaCI at pH7. The concentration was 0.4mM for free and 0.2mM in the presence of Nef. The experiments were carried out on a Bruker 600MH-izspectrometer equipped with a H,{ 13 C/l5 N} triple resonance probe. The nitrogen carrier frequency offset was set to 117.Sppm, the spectral width was set to 25ppm; 128 complex points were acquired with 8 and 32 155 Chapter 4: Structure of the TCR ~-chain scans for each increment in the indirect dimension for TCR ( alone and in the presence of Nef, respectively. 4.2.7 TCR C in LMPG micelles 1-myristoyl-2-hydoxy-snglycero-3-[phospho-rac-(1-glycerol)] (LMPG, Figure 6) was purchased from Avanti polar lipids. OH H. ,OH 0~~~~~ Figure 6: LMPG The TCR ~:detergent ratio was optimized for sensitivity and resolution in 'H1 5 N-HSQC spectra using 0.4mM '5N-labeled c-chain with an 150 to 600 fold excess of LMPG. With the optimized TCR ~:LMPG ratio, the temperature was optimized within a range of 293 to 310K using 'H, 5N-HSQC spectra. Assignment experiments were carried out using a l3 C, 5 N-labeled sample of 0.4m TCR ; in 20m phosphate buffer (pH 6.0) at 310K. 3D-HNCACB, a 3D-HNCAGO, a 3D-HCCCONH and a 3D-HCCCONH [29] were obtained with the parameters summarized in Table 2. In the HCCCONH and the HCCCONH the C TOCSY-transfer was achieved by application of a DIPSI2 cycle of 11.5ms with a 25ps pulse. F1 F2 F3 NS OFF Nuc TD SW OFF NS Nuc TD SW OFF Nuc TD HNCACB 1H 1024 14 4.7 15N 48 23 117.5 13C 80 60 43 16 HNCACO 1H 1024 14 4.7 15N 48 23 117.5 13C 100 6 174 8 HCCCONH H 4.7 4.7 36 48 23 21.5 117.5 117.5 13C 80 64 65 6 40 IH 14 14 15N HCCCONH 1024 1024 16 16 Table 2: Backdebor assigm 15N expemns for CR SW 1H botm to LMPG. The the cwlc pom (D) and iespearalueidh (S W and ie mer p aregiun tagedr wth the mniber cf trarw& atardieftr airfor hinm 156 (FF) (NS). inppnfr 3 deae mides (Nu, the mw-er f ai izon cf the cXm Chapter 4: Structure of the TCR C-chain 4.3 RESULTS 4.3.2 TCR g in solution 4.3.2.1 Backbone Assignment The optimal temperature for NMR backbone assignment experiments on free TCR ~ was assessed 1 5 N-HSQC spectra. from the general appearance as well as the sensitivity of H, Inspection of a temperature range between 278K and 310K resulted in a continuous worsening of the sensitivity with increasing temperatures. Figure 7 shows Hl,N-correlation spectra (HSQQ) at 278K and 310K, demonstrating overall decreased resolution and sensitivity due to resonance broadening at higher temperature. In addition, some resonances have broadened to a point where they are hardly detectable at all. Taking into consideration that the spectrum at 310K has been obtained with double the number of scans, the signal to noise ratio is around 6 times higher at 278K than at 310K. [ppm] 15 GLY -. .~~~~~~~ . [ppm] 15 N 110.00 N - 110.00 . II, 1 O s. a .2..... LA: - ._ .--- , . - 115.00 120.00 - 120.00 .- o. .' . -115.00 :: ,eh -:. 310-4 a _ . ^~~~~ P VW- A. .:! -125.00 't,~ -'-- 310K 278K I I 9.00 . ... I . 8.50 . 125.00 a . . J . 8.00 , . . . . . 7.50 . . . . - . 7.00 1 . . 9.00 . . . . I 8.50 .... I I I I 8.00 I 7.50 1H H [ppm] ' ' 7.00 [ppm] Figure Z7:H, 5N HSQCspra qffie TCR (at 278K(lefi)and 310K(nit). Typia speatralrgiamfor sddcti arno ads and the sidedain animog a iated by gy shadig R msati monares tdt are akerMdat hi&r tetrature am reira by armz. The spetm nat 278K hs beenobaird uth 4, the oneat 310 K uth 8 tramentsper tin nEt 1D-slics hu a di reslud d residuedwmtratethelasinsigml to nseratioathigber tneratue 157 Chapter4: Structure of the TCR C-chain Despite the aforementioned disadvantages, early assignment experiments have been carried out at 310K in order to obtain a resonance assignment of free TCR ( at the same temperature as for TCR 4/LMPG, for which 310K is optimal (see below). Since the assignment could, however, not be completed at higher temperature, additional measurements at 278K were carried out. Therefore, in the assignment process, spectra at both temperatures have been used, which have been related by a acquisition of a temperature series of H,1 5N-HSQC spectra in recorded in intervals of 1 to 2 degrees and tracing of the 1H and 15N shifts of every resonance. The extremely small dispersion of only around lppm in the H dimension (Figure 7) lends further proof to the assumed physiologically unfolded state of TCR 4. While the narrow chemical shift range enhances resonance overlap, the unstructured state is advantageous for the assignment, since random coil chemical shifts can be exploited. Accordingly, certain amino acids such as glycine, serine and threonine and alanine are resolved from the other amino acids already in the 'H, 5N- HSQC (Figure 7). This tentative assignment however, is only adduced in support of the backbone assignment based on a 3D-HNCACB, a 3D-HNCOCO and a 3D-HCCCONH (Figure 5). [ppm] 13 c 20 30 40 50 60 9 hzawebeen Figure : Stps fitn the 3DHNCA CB offiwe TCR 4at 278K For residues72 to 79 the HN-C ps by the basis of the assigmnt strategyin dhisspae,'nare a extraa d The sa ontidi ard i-1 peaks, ubi& atnst horizl bas. Intraresidualresonancs are la by gr lettens. 158 Chapter4: Structure of the TCR C-chain Figure 8 shows slices of the N-C planes of residues 72 to 79 in the HNCACB. At the position of every N-H moiety, the respective C~ and C_ resonances as well as the ones of the preceding residue are visible. CQ,and Co resonances can be distinguished by their opposite sign. The HNCACB sequence stretch depicted in Figure 8 can be readily assigned to residues 72 to 79 due to the presence of two alanines, which are one residue apart from each other, followed by a serine and a glycine at a distance of one and four residue(s), respectively. In contrast, especially for regions with the same or similar amino acids, the amino acid type sensitivity of the HNCACB renders it insufficient for an unambiguous assignment. Thus, due to resonance overlap, residues 31 to 35 (sequence RREEY) do not show any sequential peaks in the HNCACB (Figure 9, left). HNCACB . ._ t, P.., p5. .:,.. HCCCONH HNCOCO ._ [ppm] (ppm] 13c 13 [ppm] c Il -20 2.0 i,89f+ 7.1 - 30 .9 170 0 C 40 3.0 CP si 171 -50 a a -a 1H I yR 4.0 -60 R R E 31 a..__ - E Y -_-- 172 35 31 .3 z Jo l M7a Figure 9: StrPsfin t HN-Cplanesef dx 3D-MNCA CB (left), dhe 3DHN( (idde) and thdx 3DHCCCXNH ffi 7CR ¢ TYlxawtks in d HNCA CB and de HNCOX arela1w by gk lett'for dx alit ca, ,m andpntormand"C "forthe as. 7x spinssten the m peapran w addas odad i theHCCCONH am amradl by datedIis and kddai byge lette The maId "znai5 in theHNCXX) are iad by solid 1 ls. Thepsitzon f themissingC reswm'of residue Y35 in the HN4CACB is laid by a drde and t nurks. TheHNCA CB hasbeendaid at 278K theHN(C and theHCCCONHhaw bheen rewda at 310K 159 Chapter 4: Structure of the TCR C-chain In addition, in the case of residue Y35, the resonances are too weak to be detected. The same (Figure 9, middle), which sequence stretch can be easily assigned with the help of a 3D-HNCOCO connects the carbonyl resonance of a residue with the carbonyl of both the preceding and the following residue (Figure 5). In contrast to the C and C4 chemical shift, the C is much less amino acid specific. Apart from that, the connectivity in the HNCOCO is established through different scalar coupling) resulting in scalar coupling) than in the HNCACB (C-C interactions (C-C different transfer efficiencies. Therefore, while residue Y35, which does not show cross peaks in the HNCACB, it can be sequentially assigned in the HNCOCO. Additional certainty about the amino (Figure 5), in which the complete carbon spin- acid type can be received from the 3D-HCCCONH system of the preceding amino acid is obtained at the position of every NH moiety (Figure 9, right). With the sequential information contained in the three aforementioned spectra, the backbone resonances (H, N, C, C) and the Cp of all but three residues of free TCR 4-chain could be assigned at 278K (Figure 10). ITAM1 A....... ITAM2 ....... .......... ' . . 10 .. '_ _- ' 1 ' . . . ''''I.' ....... . 30 20 I 40 50 ITAM3 _ Muzzan"a 80 80 70 I 90 110 100 [ppm] G88 G49 is N G50 G30 G91 G95 G81 -G43 ;&G60 -110 G19 G86 ,,~G78 I I 8.5 I I I 8.0 8 .0 F - T I I I 7.5 H [ppm] Figurwe10: Resonaneassigmrnt offie TCR ; at 278K Thegry shad resides in the sepw by a grey im b wRned rsdai Aztwi shading 12dd add nt eyassz Reosnau assigmntsfbr e 12 nowtemisn1 areshozmin an ZH,15N-HSQC 160 hae baeen assig, tentratwy asti do Chapter4: Structure of the TCR -chain N63 was tentatively assigned, while E64 and L27 could not be assigned at all, since the resonances were missing from the spectra. The assignment hence is complete in the sense that all the assignable resonances have been also assigned, while residues that could not be assigned, do not show resonances of sufficient sensitivity in the spectra. At 310K, the assignment is less complete, since a number of resonances are significantly weakened. The backbone assignment at both temperatures is summarized in the Appendix (Section A4; Table A2&A3). Figure 10 shows the assignment of the 12 non-terminal glycines in the upfield region of the H,1 5 N-HSQC, demonstrating that also in this comparatively resolved region resonance overlap is severe in unfolded TCR C. For residues R4 to K6 and the Gterminal R115, a second set of resonances of minor intensity has been identified (Figure 11), indicating the presence of two different conformations for the two termini. While the two resonances for R115 can be readily explained by cis-trans isomerization of the adjacent proline P114, the two sets of resonances in the N-terminal region are proof for the presence of non-random-coil structure in this region, because at least one set of resonances has to arise from a structural arrangement different from random coil. The existence of two sets of resonances for this region demonstrates that the conversion between the two conformations either takes place on a slow time-scale or they represent two species of TCR ~ altogether. The two conformations are present over the whole temperature range (Figure 11) and exhibit about the same relative orientation [ppm] [ppm] sN F7 15N OO 122 123 123 L3 0 O~ 124 o~~ 124 O°1 K6O~o 00*4O 125 K62 125 RiIS 126 278K .II. . 8.4 126 R1152 .......... . 8.2 . . 8.0 . . . 7.8 'H [ppm] 8.6 8.4 8.2 8.0 7.8 'H [ppm] Figure 11:SeaMionvmte 'H,'NHSQC f CR at 278K(left)and310K (it). Theto setsof rsona forR4K6andRl 5are laed Thes i esnm of L3 andF7amalso imt A t 310K the onanme of L3, 'vbid appears atlouer hs5 is idicated by an asterisk. 161 Chapter 4: Structure of the TCR C-chain 4.3.2.2 /Nef-interaction The residues of TCR ~ involved in Nef-binding have been determined by adding unlabeled Nef to 5 N labeled TCR ~ and comparison of the 'H 5N-HSQC of the bound and free TCR 4-chain (Figure 12, above). While most of the resonances remain at the same position, some are shifted upon Nef binding to a varying degree. This demonstrates that Nef is binding to the ~-chain. In the Nef-bound spectrum of TCR C, a number of resonances have shifted to an extent that they cannot be related to a resonance in the free state (Figure 12, resonances labeled by an asterisk). Unfortunately, the identity of these residues cannot be elucidated since no assignment of TCR bound to Nef is available. The quantitative interpretation of chemical shift changes as indicators for the strength of an interaction may however be misleading in any case, since chemical shift changes reflect alterations in the chemical environment, the extent of which might not be correlated directly to the extent of involvement in a binding event. In case of an unfolded protein like TCR C, the correlation is, however, more direct than for a folded molecule, where internal conformational rearrangements might complicate the identification of an interaction site. Based on a semi- quantitative chemical shift analysis (Figure 12, below), two interaction sites of TCR 4 with Nef can be identified, residues 4 to 15 and 51 to 58. A third stretch of minor chemical shift changes is located at residue positions 41 through 43. In addition, small chemical shift changes are present along almost the whole sequence. For residues V5 and K6 both sets of resonances exhibit the same extent of peak shifts. Due to spectral overlap, resonance shift upon binding cannot be followed for the second conformation of R4. Most of the observable residues (all residues besides prolines, which cannot be detected in a H',N-HSQC, since they do not possess an amide proton) within the two major interaction regions exhibit resonance displacements to a degree that the resonance in the Nef-bound state is so far shifted from the free form that it could not be identified. These resonances are assigned in the 1 H, 5N-HSQC (Figure 12, above). 162 Chapter 4: Structure of the TCR 4-chain l Cm C [ppm] 5N 000 110 AM 115 S gr D12 a a 40* S i m *n N el 120 K55; aw * Amb All A13 ,-Vm K6 4 -_ ; Vt! * *'D alwt 125 A m to H [ppm] 8.50 ITAM1 .ITAM2 ITAM3 di C 0 x 0 0 U) Ca b- ala I ILbLngLjiLna 20 40 60 Residue A 03 o 80 Figure 12: Caption cat on the rnext paE 163 100 dL Chapter 4: Structure of the TCR 4-chain Figure 12 (pl vious page): to uwad /Nfineraction A hbe 1H, 5N-HSQCglffieeTCR (auk) and 15N-lah Nef(gry) at 293K A 2:1 excessofNef has beenused at 0.2 nM TCR dAnial shift fm ro indfie m between the o states,are assigec ew state,a itiatd byasks. leering in theyaxis signifihedfiula owdappt nvmetan hlf Nef-bwrl fr onrnepcssiW.d: ntoap esid , fuhiab noshft Belowsen-qn i d . Resaym, ich exhibit extemiiw xr state, vz caoyx be dated to sbft oti qmn Nefbiaig The shiftsbetueenthe maunms ffim ;and 4At=7dto Nef a: extnt ofrese el b: owda reswa in the Nef g ls dan hdf cowArfc: notoziappungdse tier, far aatt,nti d lfeid ersitx b 4dbad d f theNyn t on , notpsi Iide can ofbA ,o barisgiw -spes ,ote at dx sanrpitiomorte ,d e isaprdim These results demonstrate unambiguouslythat Nef binds to the cytoplasmicdomain of the T-cell receptor C-chain.Furthermore, the interaction is restricted to two distinct regions of TCR C, while the rest of remains unperturbed, indicating specific, localized binding rather than an overall structural transition. With all care with respect to the interpretation of the NMR data, it has to be noted that neither of the three ITAM sequences is involved in the interaction. This disagrees with previous biochemical data published in the Reinhart-group [3] (Figure 13). In addition, no elevated chemical shift changes are detected in the region of either binding site determined in the mutagenesis study. Several explanations can account for the deviating results of the NMR and the mutagenesis study. The observed differences could arise from the comparison of two different techniques, which observe different parameters as probes for binding. The mutagenesis study is based on the detection of binding events in a yeast-two hybrid assay [3]. In this in zw assay, it is possible that a number of events could impair the 4/Nef-interaction such as alternate interactions or steric considerations. 4 15 51 N .ITA.-A 24 58 I 01131111111011PW .~ ITM21.T 2:. 34 74 ;1 :.AM?3: t C 79 Figuw 1L3Nef btig sitesof TCR Thetwo jor interaeions kts doby the NMR imiestion areshonmate thesmzutic senpm Theanr add squaes aregm rtesides,for h signifant dnrical shiftdAr addbe idef qp Nefbing amhilid 7heNfi eractionsitentfeier 164 are dicated owthesenm& Chapter 4: Structure of the TCR C-chain On the NMR side, the aforementioned possible indirect nature of NMR chemical shift perturbations can result in differences between the detected and the actual binding site in these experiments, especially since only the backbone amides have been investigated, while no information on the side chains could be obtained. Thus, Nef binding at the positions identified within the mutagenesis study might not be accompanied by changes of the chemical environment to an extent to which secondary conformational changes affect the regions identified by the NMR analysis. While this constitutes a possible explanation for the absence of chemical shift changes in putative binding regions, regions exhibiting chemical shift changes are still involved in the binding event. A different explanation could be found that although both studies focus on the TCR ~ cytoplasmic domain, the chemical shift perturbation study has been carried out on the isolated cytoplasmic domain in solution (with three nucleotides of the transmembrane domain added to the N-terminus). It is questionable if the interaction of Nef with the N-terminus of the TCR ~ cytoplasmicdomain is biologically relevant as identified in the NMR-study, since this interaction would be most likely by the presence of the cell membrane sterically complicated under physiological conditions. Hence, the sterical accessibility of the N-terminus in our study could offer an additional non-physiological binding site for Nef. Although both the TCR ~ cytoplasmic domain and Nef have been studied as fusion proteins in the mutagenesis study, the presence of an additional protein at the N-terminus should not interfere with Nef binding at the N-terminus since the two components of the fusion protein are not directly attached to each other but separated by a putatively unstructured linker region. It is possible, however, that apart from steric considerations, conformational freedom is crucial for Nef binding to the N-terminus in the NMR study. On the other hand, it could also be that involvement of both TCR 4 and Nef in fusion proteins causes changes in Nef binding from the physiological situation. Apart from this explanations, the differences in the Nef binding sites can also arise from the intrinsic propensity of TCR ~ to dimerize, which has been reported only recently by our co-workers [5]. Gel filtration and dynamic light scattering experiments support that the TCR cytoplasmic domain is present as a dimer at the concentration and temperature used in the Nef binding study. So far, it is unknown whether Nef binds to TCR ~ in its monomeric or dimeric form. The strength of the ;/Nef-interaction (KD=0.3-2pM) is slightly higher as the one reported for the C/ interaction 165 Chapter4: Structure of the TCR 4-chain (KD-10LM), indicatingthat disruption of the ,/ dimer by binding of Nef to the monomeric species can take place at the concentrations studied (twofold excess of Nef). If Nef binds to the monomer, chemical shift perturbations are expected both within the dimerization interface and within the Nef interaction sites. Even if Nef is binding to the /~-dimer, the observed chemical shift perturbations could arise from conformational changes within the dimer upon Nef binding as well as from direct interactions with Nef. 4.3.2.3 q/-Dimerization In order to dissect possible monomer-dimer transitions from Nef binding, both the C/4-dimer and the C-monomer need to be NMR-spectroscopically characterized at the conditions of the ~/Nefinteraction study (293K, pH7). A first attempt to achieve this has been a concentration dependent chemical shift analysis. In the presence of 100mM NaC1 as it is the case in the ~/Nef-binding study, the KD of the 4/4-interaction amounts to about -10[tM [5]. These conditions are unfortunately well beneath the concentrations that can be studied by NMR. However, according to our co-workers, the KD of C/4-dimerization increases to around 3001 tM at lower salt conditions. Therefore, '-L 5N- HSQC spectra at 400pM and 10[iM of TCR 4 under low salt conditions (no NaCL was added to the sample) were investigated for chemical shift changes (Figure 14). In general, only very slight deviations in the chemical shifts could be detected in these experiments. In particular, the 'H chemical shift changes are so minute (on average 0.003 +0.00lppm) that they have been disregarded in the further analysis. From the analysis of l5N chemical shift perturbations, only the region between residue 24 and 42 exhibits concerted changes (Ab-S -0.08 ppm for seven out of the 19 residues). This region is, however, far away from the interaction sites with Nef. Of the two single residues with elevated chemical shift changes, R4 and Q94, the former one constitutes a part of the binding interface to Nef. It is remarkable that all the resonances of the second conformation of residues R4 to K6 exhibit large concentration dependent chemical shift changes (Figure 14). Apart from the concentration dependence, the monomer-dimer equilibrium is also dependent on temperature. Therefore, the temperature dependent 'Hl 5N-HSQC series used to transfer the assignment at 278K to the one at 310K has been also analyzed for the extent of chemical shift changes (Figure 15). The observed temperature dependent chemical shift changes are about one order of magnitude higher for "5N and two orders higher for 1H than the concentration dependent ones. Therefore, both nuclei are considered in the chemical shift analysis in this case. 166 Chapter 4: Structure of the TCR -chain [ppm] 4a OW 15N 112 T100 * _ 114 a0 116 o o *: S10 ~ e 118 R41a R 4 l-%,.h Y24 a ,_l"a-,N25 _ - _* ~~ F a W4 ll L3 v a © [' L62 ~L61. D39R42 e R41- 11 *S MM9L624R115* R11 R115 ~ a _ 400 tM 122 124 '0 a 120 126 i I 8.4 8.6 W 1H ITAM2 ITAM1 0.15 .0 m 8.2 [ppm] ITAM3 0.1- z (O 0.05 -l - 020 40 60 Residue 80 100 4-6 2"~ Conf. at 400pM (badk) and di ntrizationstudiesqfthe -dain. H,l5N-HSQC spectra 14: Conntration (ubs) as pltd againstthe cl shiftdf 10OpM (grey);-aweration at 293K are ozwlaL A bsolute15N Figur reide m c v bow the spectn Theputatze dn zation site i ndicataed by greyshadirg. CQeia sht dhans for the by hig esabi than 005 ppm a la secand set of resonancrsf residue4 to 6 are also gizen Residuh arrw. Peaks, vh appearat lozer co ration, are indicatedby asteriks; shiftingresdu am assigr 167 Chapter4: Structure of the TCR -chain - [ppm] 15 G95 - _ .. N G78 I _1 1 -112 W .... "JIA-. _r T03 ,, - _ -114 T100 310K T98 8.2 8.0 8.4 8. 4 278K I HI ppm] ppm] I[ :.. 1 (a co &Z 0.5 0 WV . ., .¢ -. '.' ITAMI !:.-:^ i. 0.2 D '_ ;~~ :, ., ,. ' '.: i.: : 0 -' "-, I..;' 11 20 d w1 _...11: .111111 60 40 dim "":i:~- triznstdi f te 4-dh. . . I .... .. . I ,i '' . '', . '., I:. . '. I :.' ". :., ':: - !: ' ll1: ."l 11|. w 11: w: :11 1 w111 w: w 80 100 Residue Figuw 15: Tpramre ' ':, . < 0.1 .. -:/ 1IM2 _ ,.,... .. '. ....'.' ., '.!.,-:v : 4-6 2 nd The e Conf. and so/,rediem mg q IH,15N residuff are assid HSQC speara at 278, 283, 293 and 310K (Hade to lightgmey)are ozeda) Resdzlid exera the checal shift dmngsuponteqratue ire H and 15N dreical shift dn spertra at 278 and 310K (Aoa are idicateduith arr. bs) and kzen the 15Ndxnmiadshiftd and (ab(A H - nAcean)) ibdow d speno N~~~ // arepki agiimsttheresidemir s amplktd as absdlutewes. A eragedx l shf dms am reidiated by dd hozvtld I. Reo' ted highdxcniashif echibiti dh am higlited 168 Chapter 4: Structure of the TCR C-chain While "5 N resonances show both positive and negative chemical shift changes upon increase of temperature, the imino-protons exhibit concerted downfield shifts. This is due to their dependence on the exchange rate with the solvent water in addition to their conformational dependence. Accordingly, the total H chemical shift changes have been not been interpreted directly but the absolute deviation from the mean chemical shift changes have been considered as a measure for conformational changes. In addition, proton chemical shift perturbations are evaluated only in support of the "5N data or in cases of extreme deviations. Four regions with elevated "5 N chemical shift changes are observed (residues 4-10, 16-17, 37-40 and 100-108); a fith putative dimerization region can be identified at sequence positions 93 to 95 based on an extreme H chemical shift change of 0.5 ppm for G95 and elevated "5 N chemical shift changes for Q94 and Y93. While the regions between residues 37 and 40 and 93 to 94 coincide with the putative dimerization site identified bythe concentration dependent chemical shift changes, the N-terminal region (4-10) constitutes a part of the identified Nef binding site. In contrast, the region between residue 100 and 108 has not been detected in either other study. 4.3.3 TCR Cbound to LMPG-micelles Prior to the structural investigation of the LMPG-bound TCR (, the :LMPG ratio was optimized by analysis of the resolution and sensitivity in H,'5 N-HSQC spectra with protein:detergent ratios between 1:150 and 1:600. A 300fold excess of LMPG to TCR ; was found to be optimal at a 0.4 mM concentration of the TCR ( (data not shown). Temperature optimization in the same fashion yielded 310K as optimal. As demonstrated in (Figure 16, left) for the glycine region at 310K and 318K, the sensitivity is significantly decreased at temperatures higher than 310K due to more dramatic line-broadening. At lower temperatures (data not shown), sensitivity goes down as well. Higher temperatures are favorable due to a decrease in viscosity resulting in line-narrowing. At temperatures higher than 310K, however, the benefit of lower viscosity is counteracted by another effect, possibly thermal disruption of the detergent micellesor increased exchange processes of TCR C, leading to increased line-broadening. Therefore, the structural investigation was carried out at 310K. The 1 H, 5 N-HSQC of TCR ~ in the presence of LMPmG-icelles compared to free TCR ~ exhibits strongly increased line-widths (Figure 16, ight) at only slightly increased spectral dispersion, leading to a dramatic decrease in resolution. 169 Chapter 4: Structure of the TCR -chain [ppm] 310K N -100 08 %, .. ( ppm] + LMPG free N ~~~~~~~~~~110.00 ,~~~~~~~~~~~~. am109.00 -110.00 8.60 318K 8.40 115.00 8.20 'H ppm] 318K >,,r . [ppm]oX~s N 120.00 108. 00 109.00 . 125.00 -110.00 i 8.60 l l l l l l ,I ,.,,,,,,.,, ,,, I~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~~,, i 8.40 i i i , . . . . . . . . . . . . ....i.. 9.00 8.20 H [ppm] 8.50 8.00 7.50 7.00 6.50 'H ppm] Figure 16: 7TCR bwd to LMPG ridla. Left G*wd gin of H,5N-HSQC spera of LMPGbkma TCR at 31 K(top)and 318K(bttar). Right 'H,1 5N-HSQCspera cffr 7CR (iac) and 7R boid to LMPG nidles (gry) at 310K The similarity in resonance positions between free and micelle-bound TCR ~ is minimal, signifying an overall structural rearrangement upon micelle-interaction. The backbone assignment of detergent-bound TCR ~ has been based on a 3D-HNCACB and a 3D-HNCACO. Residue type specific assignments were extracted from a 3D-HCCONH and a 3D- HCCCONH. The two partly redundant TOCSY experiments were obtained for the subsequently planned side-chain assignment. The less informative 3D-HNCAGO (Figure 5) had to replace the 3DHNCOCO in this case, since the association with the detergent micelle increased the relaxation of TCR ~ and the longer 3D-HNCOQ sequence could no longer be carried out with sufficient sensitivity. The resonances show widely varying intensities in the spectra. Thus, several stretches could be readily assigned from the connective information of the HNCACB and the HNCAQO alone, as shown for residues 33 to 41 in Figure 17 to the left. 170 Chapter 4: Structure of the TCR 4-chain HNCACB HNCACB [ppm] 13 HCCCONH ... I P..P . C -......... [ppm] J1 .tIb:PA#Zt 13 - ':3''# 40.00 *444'!1k? - 40.00 cc OC"'%~ - 50.00 am 4z Is ...a -9 -4 HC HX 50.00 OC P. - 60.00 E E y D V 33 .. D K R Cx H 41 G L D Y 88 Q [ppm] [ppm] 13 13 c C SC' 'f H 'D G YQI 175.00 " ;~i,- -- O HDGLYQ~° D EEYDVLDKR0 94 HNCACO HNCACO 33 - 60.00 1 41 ~ 88 175.00 176.00 94 Figure 17: Spectrausedfor the assignmnt qf TCR bmid to LMPG. Left Stripsforn e HN-C plane of reside 33 to 41 fromthe 3D-HNCA CB (top) and the 3D-HNCA CO (btt; i to i-1 mmotiies are inicated by horizornalbas. Right. Owa stips from the hN-C planes of residue89 to 94 of the 3D-HNCA CB (ba contcars)and the 3DHCCCONH (greyoonts) (t) and the 3D--HNCA (kbon); i to iiities uithin the HNCA CB ae indicated by dotted lis, c thoe that dd only he established based on the HCCCCONH are gizen by solid lines. The I to i- 1 zmctiuty in the HNCA CO is indicatedby a sdolidline In contrast, in other regions, both the HNCACB and to an even higher degree the HNCACO show only the strongly weakened intraresidual peaks (Figure 17, right), with i-1 peaks that, if they are present at all, are only visible upon meticulous analysis of the respective 1-D slices. In these cases, mainly the strong C' resonances in the HCCCONH have been used to establish connectivity, which were then verified in the HNCACB. This strategy is demonstrated in the right part of Figure 17, where strips from the HNCACB and the HCCCONH are overlayed. In addition to stretches of weak resonances in the assignment, a number of resonances could not be assigned or were missing from the spectra entirely. As a consequence, 14 residues are missing entirely from the final backbone assignment (Figure 18) and an additional 5 residues could only be tentatively assigned. The assignment is summarized in the Appendix (Section A4; Table A4). 171 Chapter 4: Structure of the TCR C-chain ITAM1 GR " . . . ITAM3 ITAM2 70 Figure 18: Badek 60 50 40 30 20 10 80 resane 100 90 assignmrntq t he TCUR bKoz to LMPG-i. assig' wdediw esidues not id lyassig' tmaedy assiresi 110 The residu shadl in grey dld te s are la gh ey aces. The chemical shift indices (CSI) for H, chemical shift perturbations from random coil chemical shifts [30] have been used to investigate the presence of secondary structure within the assigned regions of LMPG-bound TCR ~ as reported from CD-experiments [1]. While regions of at least 4 consecutive residues exhibiting a CSI of +1 are indicative for 3-sheet conformation, stretches with a CSI of -1 report on an a-helical arrangement [30]. For the regions of LMPG-bound TCR C, for which a HL chemical shift could be obtained from the HCCOC)NH, no evidences for any secondary structure can be observed (Figure 19). Therefore, it is concluded that the helical regions have to be located within the areas of TCR C, which are unassignable in the NMR spectra due to extensive resonance broadening, namely residues within or adjacent to the ITAM2 and ITAM3. These regions also coincide with the longest stretches of predicted a-helical structure based on the primary sequence as predicted by the program PSIpred. Therefore, it is proposed that the regions around ITAM2 and ITAM3 adopt helical structure upon interaction with the lipid micelle Sequence ITAM1 ITAM2 ITAM .S.'AYGMGERRRCKGHDLYQG-/ALHM2APPR 'N& GSLRVKFSRSADAPAYQQGgNQLYNELNLGRREEYDVLDRRGRDPEM(KGKPRRKNPQEGLYN 1'0 20 30 40 50 60 70 do go 100 110 Prediction Chemical shift Index 3?111H 01 -1 1 11" L| l I I fthe aws sible gm fLMPGbwd TCR 4, thesemnarystnamepw tdbyPSIpred based Figure 19:Alit on d aino acidsauere and CSI aniis of dxeHa dial shifts.Ha dxnil shiftshae beenextratedfian dx 39 HCCCNH spean Next reibor dependt randomai dxnial shiftshae beenobtaid fro theprogramNMRuew +0.1ppmnrults in a dxnial shif firn therandomail due er thadn detiaim of dxeecxit [31, 32]. Positiwe of eier sign,the CSI is 0. mrthan-0.ppmrsul ina CSI of -1,forsnerdeiat CSI f +1, regaiw deiat i etem elHadnicd shot bysmll ban. fiantede Rfidues uith a CSI q0 hazebeen di 172 Chapter 4: Structure of the TCR 4-chain Since the parts of the protein, containing two of the three interesting ITAM motifs could not be assigned and the Ha chemical shift analysis does not indicate the presence of secondary structure elements within the assigned parts of the sequence, any further structural investigation on LMPIVGbound TCR ~ was abolished. The increase in line-width in or adjacent to ITAM2 and ITAM3 of LMPG-bound TCR C, which impairs resonance assignment, however, carries structural information on its onw. The line-width of a resonance is determined by its transversal relaxation rate, which is sensitive on the one hand to slow exchange processes and on the other hand to fast molecular reorientation events. Thus, an increase in line-width signifies the presence of increased conformational exchange or the involvement in a structural arrangement of increased molecular reorientation times, e. g. micelle incorporation. The increased line-width of all resonances of TCR ; in the presence of LMPG as compared to free TCR reflects involvement with the detergent micelles. The additionally broadened resonances in the region of ITAM2 and ITAM3 allow for different ~/micelle interaction models (Figure 20): The regions of TCR C,which exhibit increased line-broadening, could be stably associated with the LMPG-micelle (Figure 20A). Consequently, these residues experience the increased reorientation times of the micelle leading to line-broadening, while the remainder of TCR ~ is going in and out of it or just moving freely in the solution. An alternative explanation is that the two ITAM regions are exchanging between different lipid bound forms (Figure 20B) or a lipid bound and a free form (Figure 20Q), thus causing exchange broadening of the concerned resonances, whereas the remainder of TCR ~ protrudes freely into solution. The first hypothesis is unlikely, considering that extremely modest changes in relaxation behavior have been reported for proteins of the size of TCR ; when incorporated into LMPG-micelles [33]. In this earlier investigation, the micelle bound form of a 12 kDa protein showed the relaxation behavior of a 20 kDa molecule and exhibited correspondingly narrow line-widths. It is reasonable to assume that C, which possesses a molecular weight of around 13 kDa, exhibits a similar relaxation behavior. Therefore, a conformational exchange model for the TCR /LMPG-micelle interaction (Figure 20) is more likely. While the conformational rearrangement on the LMPG-micelle (Figure 20B) would not necessarily be accompanied by changes in the TCR 4 secondary structure, the exchange between a micelle-bound and a free form (Figure 20,C) includes changes from a helical to a random coil structure in the regions of ITAM2 and ITAM3. 173 Chapter 4: Structure of the TCR 4-chain A B _ is ij' -p - )t .- 00 A-40- N Figure 20:Modiesqf T/LM PGnicde eraaid 4.4 CONCLUSIONS In the course of this work, the backbone assignmentof both the free TCR ~ and TCR 4 bound to LMPG-micelles has been achieved. The almost complete assignment of the free form provides an NMR spectroscopic fingerprint, which constitutes the outset of a residue specific investigation of the binding site of SIV Nef. In order to identify this binding site, however, the TCR ~/Nef-interaction sites have to be dissected from the ones of the C interaction. While the conditions, under which the TCR 4/Nef-interaction of a studies as well as the assignment experiments were carried out, are in favor /4-dimer, the 4 monomer has so far not been characterized NMR spectroscopically. First concentration as well as temperature dependent investigations aimed at the identification of the C/4interaction sites as well as at characterization of the monomeric species, have proven partly incongruent. So far, only minute changes could be identified in the concentration dependent study, while a number of putative interaction regions could be identified by the temperature dependent experiments. Temperature dependent chemical shift changes can, however, arise from reasons other 174 Chapter 4: Structure of the TCR C-chain than changes in the 4/-interaction, since the conformational ensemble defining the chemical shift of a spin in an unfolded protein such as TCR ~ can change with temperature due to different energy barriers for different conformational states within the ensemble. In the case of the imino protons, solvent exchange influences the chemical shift in addition to conformational aspects. In addition, no defined end point was reached at higher temperature in the investigated temperature region from 278K to 310K, signifying that the experiment failed to achieve conditions, under which the pure monomer could be NMR spectroscopically characterized. From the unsuccessful concentration dependent experiments, which have been carried out at the same temperature as the /Nef- interaction study, it seems to be impossible to obtain a spectrum of the monomer at these conditions. Therefore, further studies will aim at a conclusive characterization of the 4/-interaction site(s) by concentration dependent studies at higher temperatures, where the monomer-dimer transition is shifted to higher concentrations. Even under the optimized conditions in regard to the TCR (:LMPG ratio and the temperature, the backbone assignment of TCR ( bound to LMPG-micellescould not be completed due to extensive broadening of a number of resonances. Because of this incomplete assignment, the structural investigation of LMPG-bound TCR ( was not carried any further than the backbone assignment. Structural information could however still be obtained for both the assignableand the unassignable regions. A chemical shift analysis measuring deviations from the random coil chemical shifts as an indicator for the presence of secondary structure demonstrate that the assignable regions do neither adopt a-helical nor P-sheet structure. Consequently,the detected a-helical content of TCR ( upon micelle-binding has to be located within the non-assignable, broadened regions, located at the 2 nd and 3r ITAM motif. This is in agreement with sequence-based secondary structure predictions. Furthermore, the increase in line-width in these regions indicates the involvement in chemical exchange processes in the millisecond range. Different interaction models with the LMPG micelle have been proposed here, which are in agreement with the localized occurrence of elevated slow exchange (Figure 20). In conclusion, the study demonstrates that only the regions around ITAM2 and ITAM3 (and not ITAM1) can adopt a-helical structure. These regions are also the most likely interaction sites with the LNPG micelle. 175 Chapter4: Structure of the TCR c-chain 4.5 REFERENCES 1. Aivazian, D. and Stem, L. J. (2000). Phosphorylation of T cell receptor zeta is regulated by a lipid dependent folding transition. Nat Seie Bid, 7, 1023-1026. 2. 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K.; Theriault, K.; et al. (1995). Molecular basis for interaction of the protein tyrosine kinase ZAP-70 with the T-cell receptor. Natu, 377, 32-38. 12. Samelson, L. E. (1999). Adaptor proteins and T-cell antigen receptor signaling. ProgBiqs Md Bid, 71, 393-403. 13. Clements, J. L. and Koretzky, G. A. (1999). Recent developments in lymphocyte activation: linking kinases to downstream signaling events. J COinInest, 103, 925-929. 14. Janeway, C A., Jr. (1995). Ligands for the T-cell receptor. hard times for avidity models. Inwma 15. Today, 16, 223-225. Cochran, J. R; Aivazian, D.; Cameron, T. O.; Stem, L. J. (2001). Receptor clustering and transmembrane signaling in T cells. Tmrls BiaodmSci, 26, 304-310. 176 Chapter 4: Structure of the TCR 4-chain 16. Delon, J.; Gregoire, C; Malissen, B.; Darche, S.; Lemaitre, F.; Kourilsky, P.; Abastado, J. P.; Trautmann, A. (1998). CD8 expression allows T cell signaling by monomeric peptide-MIHC complexes. In ity, 9, 467-473. 17. Grakoui, A.; Bromley, S. K.; Sumen, C; Davis, M. M.; Shaw, A. S.; Allen, P. M.; Dustin, M. L. (1999). The immunological synapse: a molecular machine controlling T cell activation. Sie7e, 285, 221-227. 18. Deacon, N. J.; Tsykin, A.; Solomon, A.; Smith, K.; Ludford-Menting, M.; Hooker, D. J.; McPhee, D. A.; Greenway, A. L.; Ellett, A; Chaffield, C; et al. (1995). Genomic structure of an attenuated quasi species of HIV- 1 from a blood transfusion donor and recipients. Sae, 270, 988-991. 19. Salghetti, S.; Mariani, R.; Skowronski, J. (1995). Human immunodeficiency virus type 1 Nef and p561ck protein-tyrosine kinase interact with a common element in CD4 cytoplasmic tail. ProcNatldA cadSci USA, 92, 349-353. 20. Baur, A. S.; Sass, G.; Laffert, B.; Willbold, D.; Cheng-Mayer, C.; Peterlin, B. M. (1997). The N-terminus of Nef from HIV- 1/SIV associateswith a protein complex containing Lck and a serine kinase. Inmoty, 6,283-291. 21. Collette, Y.; Dutartre, H; Benziane, A.; Ramos, M.; Benarous, R.; Harris, M.; Olive, D. (1996). Physical and functional interaction of Nef with Lck HIV-1 Nef-induced T-cell signaling defects. J Bid em, 271, 6333-6341. 22. Lee, C. H; Leung, B.; Lemmon, M. A.; Zheng, J.; Cowburn, D.; Kuriyan, J.; Saksela, K. (1995). A single amino acid in the SH3 domain of Hck determines its high affinity and specificity in binding to HIV- 1 Nef protein. EnboJ, 14, 5006-5015. 23. Saksela, K.; Cheng, G.; Baltimore, D. (1995). Proline-rich (PxxP) motifs in HIV-1 Nef bind to SH3 domains of a subset of Src kinases and are required for the enhanced growth of Nef+ viruses but not for down-regulation of CD4. EnidJ, 14,484-491. 24. Lu, X.; Wu, X.; Plemenitas, A.; Yu, H.; Sawai, E. T.; Abo, A.; Peterlin, B. MI.(1996). CDC42 and Racl are implicated in the activation of the Nef-associated kinase and replication of HIV-1. Curr Bid, 6, 1677-1684. 25. Greenway, A.; Azad, A.; Mills, J.; McPhee, D. (1996). Human immunodeficiencyvirus type 1 Nef binds directly to Lck and mitogen-activated protein kinase, inhibiting kinase activity. J Vita, 70, 6701-6708. 26. Sawai, E. T.; Baur, A; Struble, H; Peterlin, B. M.; Levy, J. A; Cheng-Mayer, C (1994). Human immunodeficiency virus type 1 Nef associates with a cellular serine kinase in T lymphocytes.Prc NadAcad Sci U S A, 91, 1539-1543. 27. Smith, B. L.; Krushelnycky, B. W.; Mochly-Rosen, D.; Berg, P. (1996). The HIV Nef protein associateswith protein kinase C theta. J Bid (xem 271, 16753-16757. 28. Wittekind, M. and Mueller, L. (1993). HNCACB, a High-Sensitivity 3D NMR Experiment to Correlate Amide-Proton and Nitrogen Resonances with the Alpha-Carbon and Beta-Carbon Resonances in Proteins.JMagnReonSerB, 101, 201-205. 177 Chapter4: Structure of the TCR c-chain 29. Montelione, G. T.; Lyons, B. A.; Emerson, S. D.; Tashiro, M. (1992). An Efficient Triple Resonance Experiment Using Carbon-13 Isotropic Mixing for Determining SequenceSpecific Resonance Assignments of Isotopically-Enriched Proteins. J Am Cbem Soc, 114, 10974-10975. 30. Wishart, D. S.; Sykes, B. D.; Richards, F. M. (1992). The chemical shift index: a fast and simple method for the assignment of protein secondary structure through NMR spectroscopy. B/xristry, 31. 31, 1647-1651. Schwarzinger, S.; Kroon, G. J.; Foss, T. R.; Chung, J.; Wright, P. E.; Dyson, H. J. (2001). Sequence-dependent correction of random coil NMR chemical shifts. J A m C/rn Soc, 123, 2970-2978. 32. Wishart, D. S. and Sykes, B. D. (1994). The 3 C chemical-shift index: a simple method for the identification of protein secondary structure using 13C chemical-shift data. J Bion NMR, 4, 171-180. 33. Krueger-Koplin, R. D.; Sorgen, P. L.; Krueger-Koplin, S. T.; Rivera-Torres, I. 0.; Cahill, S. M.; Hicks, D. B.; Grinius, L.; Krulwich, T. A.; Girvin, M E. (2004). An evaluation of detergents for NMR structural studies of membrane proteins. J Bion NMR, 28, 43-57. 178 Appendix APPENDIX 179 Appendix TABLE OF CONTENTS A1 CHAPTER 2: r(HCN)-Experiment A1.1 ...................................................................... 181 Pulseprogram s ........................................................................................................................181 A l.1.1 F(H .......................................................................................................................... 181 184.................................................... A1.1.2 r(H2'C', .....................................A2.1 F-rate calculation ..................................................................................................................187 A1.1.3 Source-file ......................................................................................................................188 A1.1.4 Getrate 189 frompdb.sh ................................................................................................ A1.1.5 Get_ratefrompdb.c ..................................................................................................189 Coordinate file independent -rate calculation ........................................................191 A1.1.6 195 ............................................................................................................................... A 1.2 References CHAPTER 3: RNA Tetraloop Dynamics.............................................................196 A2 A2.1 Pulse sequences ......................................................................................................................196 A2.1.1 RI .....................................................................................................................................196 A2.1.2 Rlp................................... 198 A2.1.3 "3CHetnOe ...............................................................................................................201 A2.2 Extraction of peak intensities ...............................................................................................202 A2.2.1 Autopkhpos.mac ...........................................................................................................202 A3 GHAPTER 4: Structum of the TCR c-chain ........................................................ 203 A3.1 Assignment of free TCR at 278K ....................................................................................203 A3.2 Assignment of free TCR at 317K .................................................................................... 205 A3.3 Assignment of TCR /LMPG at 310K ..............................................................................207 180 Appendix A1 CHAPTER 2: F(HCN)-Experiment Al.l Pulseprograms AI.1.l F(HCN) A1.1.1.1 Reference Experiment ;ghcn_final_ref DELTA5 (center (p2 phl) (p22 phl):f3) DELTA6 pl9:gp6 d16 4u plO:f2 4u (center (pl4:sp3 phll):f2 (p22 phl2):f3) 4u #include <Avance.incl> #include <Grad.incl> #include <Delay.incl> "p2=pl*2" "p4=p3*2" "p22=p21*2" "dO=3u" "dll=30m" "dl3=4u" 4u p2:f2 pl9 :gp6 d16 DELTA6 (center (p2 phl) (p22 phl):f3) DELTA5 (p21 phl6):f3 4u (p3 phl5):f2 d13 pl6 :gp7 d16 (p2 phl):fl (p3 phl8):f2 dO 4u plO:f2 (center (p29:sp2 phl) :f2 (p2 phl) :fl) DELTA2 p16 :gp3*EA*-l d16 plO:f3 d13 (center (pl4:sp3 phl):f2 (p30:sp9 phl):f3) d13 "in2O=in0" "d6=d4-p8/2-4u" "d20=d22-d13-p16-d16-p29-12u" "DELTA1=d22-p16-dli6" "DELTA2=d22-d16-pl6-dO-4u-p29-dl3" "DELTA3=dl3+pl6+dl6+4u" "DELTA5=d26/4" "DELTA6=d26/4-p19-d16-8u" 1 ze 2 dll do:f2 do:f3 dl (pl phi) 4u d6 plO:f2 p13:f3 (center (p2 phi) d6 UNBLKGRAD 4u p28 phi (p8:spl3 phi):f2) dl3 p2:f2 pl6:gp3*EA (pl ph2) d13 pi6:gpl d16 (p3 ph3):f2 DELTA1 pl6:gp2 d16 plO:f2 plO:f3 (center (pl4:sp3 phll):f2 (p30:sp9 phl2):f3) DELTA1 pl6:gp2 d16 d20 (p29:sp2 phl):f2 4u 4u pl2:f2 4u (center (pl phl) d4 2 (center (p phl) d4 (center (pl ph2) 4u d16 p2:f2 p3:f3 d6 pO:f2 (p3 phl3):f2 d13 pl6:gp5 d16 (p3 phl4):f2 4u (p21 phl7):f3 (center (p2 phl) d6 4u (pl phl) DELTA3 (p2 phi) d13 ;ZQ/DQ-Delay 181 ; Bloch-Siegert (p3 ph8):f2 (p4 phl):f2 (p3 ph9):f2 (p8:spl3 phl):f2) Appendix p16:gp4 d16 pll2:f2 pll6:f3 4u BLKGRAD go=2 ph31 cpd2:f2 cpd3:f3 dll do:f2 do:f3 mc #0 to 2 F1EA(igrad EA & ip9*2, idO & dd20 & ip6*2 & ip18*2 & ip3l*2) exit phl=0 ph2=1 ph3=0 ph8=0 ph9=3 0 0 0 2 2 2 2 0 2 2 3 1 1 phll=0 phl2=0 ph13=1 1 1 1 1 1 1 1 3 3 3 3 3 3 3 3 ;c13 1. puls; ph14=0 ;c13 2. puls; phl5= 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 ;c13 3. x for ref, y for cross ph16=0 2 ;n15 2. x for ref, y for cross ph17=0 ;n15 1.puls; phl8=1 ;c13 after chem. shift evolution ;y for ref, x for cross ph31=0 2 2 0 2 0 0 2 2 0 0 2 0 2 2 0 2 0 0 2 0 2 2 0 0 2 2 0 2 0 0 2 182 Appendix A1.1.1.2 Cross Experiment (p22 phi2) :f3) 4u ;ghcn_final cross #include #include #include 4u p2:f2 <Avance.incl> <Grad.incl> <Delay.incl> p19:gp6 d16 DELTA6 (center (p2 phl) (p22 phl):f3) DELTA5 (p21 phl6):f3 4u (p3 phlS) :f2 d13 p16:gp7 d16 (p2 phl):fl (p3 phl8):f2 dO 4u plO:f2 (p2 9:sp2 phl):f2 d5 (p2 phl):fl DELTA2 "p2=pl*2" "Ip4=p3*2" "p22=p21*2" "dO=3u" "dll=30m" "d13=4u" "in20=inO" "d5=d4-p29" "d6=d4-p8/2-4u" "d20=d22-d13-p16-d16-p29-12u" "DELTA1=d22-p16-dl6" "DELTA2=d22-d19-p16-dO-p2-p29-d5-4u p16:gp3*EA*-l -d13" "DELTA3=dl3+p16+dl6+4u" "DELTA5=d26/4" "DELTA6=d26/4-p19-d16-8u" d16 plO:f3 d13 (center (p14:sp3 phl):f2 1 ze d13 2 dll do:f2 do:f3 p16:gp3*EA (p30:sp 9 phl):f3) dl d16 d20 (p29:sp2 phl):f2 4u (pl phi) 4u d6 plO:f2 p3:f3 2 (center (p phl) (p8:spl3 phl):f2) d6 UNBLKGRAD 4u p28 phl 4u p2:f2 4u (center (pl phi) (p3 ph8):f2 ) d4 (center (p2 phi) (p4 phl):f2 ) d4 (center (pl ph2) (p3 ph9):f2 ) 4u d6 plO:f2 (center (p2 phi) (p8:spl3 phl):f2) d6 4u (pl phi) DELTA3 (p2 phl) d13 p16:gp4 d16 pll2:f2 pll6:f3 4u BLKGRAD go=2 ph31 cpd2:f2 cpd3:f3 dll do:f2 do:f3 mc #0 to 2 FiEA(igrad EA & ip9*2, idO & dd2 & ip6*2 & ip18*2 & ip31*2) exit d13 p2:f2 (pl ph2) d13 p16:gpl d16 (p3 ph3):f2 DELTA1 p16 :gp2 d16 plO:f2 plO:f3 (center (pl4:sp3 phll):f2 (p30:sp9 phl2):f3) DELTA1 p16 :gp2 d16 p2:f2 p3:f3 (p3 phl3):f2 d13 p16:gp5 d16 (p3 phl4):f2 4u (p21 phl7):f3 DELTA5 (center (p2 phl) DELTA6 p19 :gp6 ; Bloch-Siegert ;ZQ/DQ-Delay phl=O ph2=1 ph3=0 0 0 0 2 2 2 2 ph8= 0 2 2 ph9=3 3 1 1 (p22 phl):f3) d16 4u plO:f2 4u (center (p14:sp3 phll):f2 phll=O0 ph12=0 183 Appendix phl3=1 1 1 1 1 1 1 1 3 3 3 3 3 3 3 3 ;c13 1. puls phl4=0 ;c13 2. puls; ph15=l 1 1 1 1 1 1 1 1 1 1 1 1 1 1 1 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 ;c13 3. x for ref, y for cross ph16=1 3 ;n15 2. x for ref, y for cross ph17=0 ;n15 .puls; phl8=0 ;c13 after chem. shift A1.1.2 evolution ;y for ref, x for cross ph31=0 2 2 0 2 0 0 2 2 0 0 2 0 2 2 0 2 0 0 2 0 2 2 0 0 2 2 0 2 0 0 2 r(H2'C2',N) A1.1.2.1 Reference Experiment p16 :gpl dl6 (p3 ph3):f2 d4 plO:f3 d4 plll:fl (p26 ph26):fl DELTA1 cpdsl:fl 4u (center (p4 phl): ;ghcn_quant_c2h2_ref ;avance-version (00/10/05) #include <Avance.incl> #include Grad.incl> #include <Delay.incl> "p2=pl* 2" "Ilp4=p3*2" (p30:sp9 phl2):f3) "p22=p21*2" 4u DELTA2 p3:f3 "dlO=3u" "dll=3Om" "d12=20u" "d13=4u" (p3 phl3):f2 d5 4u do:fl (p26 ph27):fl (p21 ph14):f3 4u DELTA5 pll:fl (CENHN1 p2 phl) (p22 phl):f3 DELTA6 p19:gp6 d16 4u 4u plO:f2 (center (pl4:sp3 phll):f2 (p22 phl2):f3) 4u "in2O=in0" "dO=d22" "d20=d22-d4*2-4u" "DELTA=dlO*2+p4" "DELTA1=d22-d4*2-4u-p26" "DELTA2=d22-4u" "DELTA3=d13+p16+d16+4u" "DELTA4=d22-d13 -p16-d16-p2-d4" "DELTA5=d26/4-4u" "DELTA6=d26/4-p19-d16-8u" "d14=d4*2-p26" "d5=25m/2-p21-d26/2-p26" 4u p2:f2 p19:gp6 d16 DELTA6 (center (p2 phl) (p22 phl):f3) DELTA5 4u plll:fl (p2 1 phl6):f3 (p26 ph26):fl d5 p2:f2 cpdsl:fl 4u (p3 phl5):f2 dO plO:f3 (center (p4 phl):f (p30:sp9 phl):f3) d20 4u do:fl (p2 6 ph27):fl d14 pll:fl (p3 ph8):f2 4u p16:gp3 "12=tdl/2" 1 ze dll pll2:f2 pll6:f3 2 dll do:f2 do:f3 3m 3 dll dll 4 d12 p9:fl dl cw:fl 4u do:fl lOu pll:fl (pl phl) d4 p2:f2 p3:f3 (center (p2 phl) (p4 phlO):f2) d4 UNBLKGRAD (pl ph2) 4u 184 Appendix d16 phll=0 phl2=0 phl3=l (pl phi) d4 lOu 1111111 1111111 0020220 1111111 3 3 3 3 31111111 3 3 3 3 3 3 3333333 33333333 3 3 3 3 3 3 33333333 3 3 3 3 3 3 3333333 0002222 3 3 3 3 3 3 3 1111111 3 3 3 3 3 3 3 1111111 23333333 2 2 2 2 2 3333333 0000000 2222222 1 1 1 3 3 4u (center (p2 phl) (p4 phl8):f2) d4 lOu pll2:f2 pll6:f3 4u BLKGRAD go=2 ph31 cpd2:f2 cpd3:f3 dll do:f2 do:f3 wr #0 if #0 zd 3m ip8 lo to 3 times 2 dll dd0 dll id20 lo to 4 times 12 1 3 3 3 3 ph14=0 ph15=1 1 3 3 ph16=0 2 ph17=0 ph18=0 ph2O=2 2 2 2 2 ph26=1 ph27=3 ph31=0 2 0 0 2 0 2 2 0 exit phl=0 ph2 = 1 ph3=0 2 ph4 = 0 ph5=0 ph6=0 ph7=1 ph8=0 0 2 2 phlO=0 2202002 A1.1.2.2 Cross Experiment dll pll2:f2 pll6:f3 2 dll do:f2 do:f3 3m 3 dll dll 4 d12 p9:fl dl cw:fl 4u do:fl lOu pll:fl (pl phi) ;ghcn_quant_c2h2_cross2 ;avance-version (00/10/05) #include <Avance.incl> #include <Grad.incl> #include <Delay.incl> "p2=pl* 2 " I"p4=p3*2"1 "p22=p21* 2 " d4 p2:f2 p3:f3 (center (p2 phl) d4 UNBLKGRAD (pl ph2) 4u p16 :gpl dl6 (p3 ph3):f2 "dlO=3u" "dll=30Om' "d12=20u" "d13=4u" "in2O=in0" (p4 phlO):f2) d4 pO:f3 d4 plll:fl (p26 ph26):fl DELTA1 cpdsl:fl 4u (center (p4 phll): "dO=d22" "d20=d22-d4*2-4u" "DELTA=d1O*2+p4" "DELTA1=d22-d4*2-4u-p26" "DELTA2=d22 -4u" (p30:sp9 phl2):f3) "DELTA3=d13+p16+d16+4u "DELTA4=d22-d13 -pl6-d6-p2-d4" 4u DELTA2 p13:f3 (p3 phl3):f2 d5 4u do:fl (p26 ph27):fl (p21 phl4):f3 4u DELTA5 pll:fl (CENHN1 p2 phl) "DELTA5=d26/4 -4u" "DELTA6=d26/4-pi9-d16-8u" "d14=d4*2-p26" "d5=25m/2-p21-d26/2-p26" "dl5=25m/2-p21-d26/2-d4*2-p26" "12=tdl/2" 1 ze 185 (p22 phl):f3 Appendix ph14=0 0 0 0 2 2 2 2 ph15= 1 1 1 1 1 1 1 DELTA6 p19 :gp6 d16 4u 4u plO:f2 (center (p14:sp3 phll):f2 (p22 phl2):f3) 4u 1 1 1 1 1 1 1 1 3 3 phl6=1 cross 3 ph17=0 phl8=0 ph20=2 ph26=1 ph27=3 ph31=0 2 4u p2:f2 p19:gp6 d16 DELTA6 (center (p2 phl) (p22 phl):f3) DELTA5 4u plll:fl (p21 phl6):f3 d4 ; refocussing C2'H2' coupling d4 (p26 ph26):fl d15 p2:f2 cpdsl:fl 4u (p3 phl5):f2 dO plO:f3 (center (p4 phl):f2 (p30:sp9 phl):f3) d20 4u do:fl (p26 ph27):fl d14 pll:fl (p3 ph8):f2 4u p16:gp3 d16 (pl phl) d4 lOu 4u (center (p2 phl) (p4 phl8):f2) d4 lOu pll2:f2 pll6:f3 4u BLKGRAD go=2 ph31 cpd2:f2 cpd3:f3 dll do:f2 do:f3 wr #0 if #0 zd 3m ip8 lo to 3 times 2 dll dd0 dll id20 lo to 4 times 12 exit phl=0 ph2=l ph3=0 2 ph4=0 ph5=0 ph6=0 ph7=l ph8=0 0 2 2 phlO=0 phll=0 phl2=0 phl3= 1 1 1 1 1 11 11111111 11111111 11111111 33333333 33333333 33333333 33333333 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 3 186 3 3 3 3 3 3 3 3 3 3 3 3 3 3 11 1 11 1 ;1 x for ref, y for 3 3 3 3 3 3 3 2 2 0 2 0 0 2 0 0 2 0 2 2 0 Appendix A2.1 F-rate calculation The F-rates were calculated using the CS-tensor values and orientations and the dipole-dipole vector lengths listed in Table A1. Nucle- CS-Tensor 1l 622 633 011 022 033 otfide Adenine F rI'H',NI - 148ppm 0 Adee n DD 9 ,CSAN9 Guanine . DDCSA CSAC1'N9:4.0 N -150ppm ______ Cytidine Ni .h n ~ C2'H2',NI1/9 pDDCSA CH N _________ C1'N9:16.0 ° - 143ppm C1'N1:17.3° - 160ppm C1'N1:31.30 - 148ppm Adenine C8H8:67.4° N - 150ppm C8H8:55° - 143ppm DAN9 G nne 6/8 H6/8,Ni19 r Cytidine Cydne 1 C6H6:78.7 Uracile Adene Guann .9T, ~~ ~iDnC1 ,G Cidi 9H',CI' C1 ne 63.4ppm* C1'H1':28.60 ~ The DD, CSA NH,c Ga9H6/8,C6/8 Ciidine Gaie214ppm GuaCe Cytidine 0 C6H6:90 11 0 78.8ppm* C1'H1':116.2 ° 106.1ppm* C1'H1':79.3 ° N9H8:3.8 ° 241ppm C6 NlH6:4.7 ° N9H8:93.8 ° 152ppm N1H6:94.7 ° H6 NH' Thymine ______ 2.15 2.15 215 C 61ppm N9H8:900 N1H6 2.15 216ppm C8 C8H8:27° 128ppm N1H6:95.7 ° 136ppm C8H8:117° 42ppm NH6:90 ° 61ppm C8H8:90° C8H8 1.1 8H8:280 241ppm 141ppm C8H8:118 ° 152ppm 59ppm C8H8:90° 35ppm C6H6 1.1 238ppm° N1H6:5.7 0° 238ppm C6H6:29° 141ppm 59ppm C6H6:119 0° 128ppm C6H6:119° C6H6:90 0 42ppm C6H6:90° ipci, dipdebod lghs orthe ddcatl Frates.A ll ndVIhs haw ln extractdfiUm the programINSIGHT (n-i). The tesor zdues lae wth asteriskshaze ben taken from DFT aladations[1]. All odxr tensorshazeben obtaidfi0m nridesd in thesolidstate[2]. In the caseof urad* the tensorfor 2'dxc.ds has bn gizen 0 is the angle be n the respetiwe pa r of thedx CS-tensorand the iicatad dx &pe zaor. For all tensorsof anutic aton s,1 and S22 ae onernt zdthn the baseplane and S33 S ppriadar 1.1 N9H8:90 ° 35ppm N1H6:90 ° C6H6:29 Table A1: CS-tensors and or C6H6:168.7 C8H8 2.15 2.15 _ Adene 18116/8,C6/8 -29 1ppm C8H8:90° -311ppm 11 N9H8 N9H8 Uracile C - 199ppm C8H8:145° -218ppm C'HI' C2'H2' -28lppm C8H8:90 ° C1'Hl':81.0° J~)DCSA Gaie214ppm CH,C C1'N9:90 ° -311ppm C1'N1:90° -306ppm C1'N1:900 C1'H1':111.5 136ppm N9H8:94.8 ° C8 DDCSA DDCSA -291ppm C1'N9:106.0° -218ppm C1'N1:72.7° -228ppm C1'N1:58.70 - 198ppm C8H8:157.4° C1'H1':23.5 216ppm N9H8:4.8 ° _denin / -28 lppm C1'N9:900 63.9ppm* 79.3ppm* 108.0ppm* ° ° _ymme rl - 199ppm Lenth - 160ppm -228ppm -306ppm C6H6:83.5° C6H6:173.5 ° C6H6:90 ° 110.4ppm* 64.2ppm* 79.9ppm* C1'H1':21.5 ° C1'H1':107.7 ° C1'H1':78.2 ° ' N9HI' 64ppm* 80.5ppm* 111.2ppm* 0 C1'H1':109.1 ° ° 'H1':22.7 C1'H1':78.2 Uracile I 0 - 198ppm C1'N9:86.00 Dipole to it For the C1' tensoronly the pMedion angle orntothe Ci'-Hi bondare k 187 roen Appendix All r(HCN)-rates were calculated in an UNIX environment. The coordinates of the three 15N CS-tensor components as well as the one of the GH vectors were obtained from pdb coordinate files of the respective nucleotides. The 15 N CS-tensor was simulated by exchanging the N 1 in pyrimidines and N9 in purines by a phosphorous nucleus, which allowed for the formation of six bonds. The three additional bonds were used to model the tensor components. For every nucleotide in both C2ndo and C3-eoo conformation, 72 coordinate files were created by altering the angle stepwise by 5 degrees in order to achieve a complete 360° rotation using <name>.source file in INSIGIffII. The pdb files were numbered consecutively (format= <name ><number>.pdb). From the coordinate files, F(C1'H1',N), F(C2TH2',N) and F(C6H6,N) or F(C8H8,N) were calculated using the Gprogram get_rate_frompdb.c. The usage of this program is: get ratefrom pdb <max_number of pdb_files> <pdbfilename> The Cprogram was used in combination with a shell script (getrate_frompdb.sh) in order to input multiplepdb files. A1.1.3 Source-file Source-file for adenine. # A.source DefineMacro A Int n,m Int zl,z2,z Get Molecule Archive Frame 1 /fs/data/ric/GAMMA_HCN/SIMULATION/PDB2/B_Form/A/A.car A -ReferenceObject m= -98 Foreach $z2 From 1 To 72 Geometry Dihedral $m A:1:04' A:l:Cl' A:l:P9 A:1:C4 Put Molecule PDB a (a//$z2//.pdb) -Transformed -Displayed -InsightStyle m = $m + 5 End End Macro 188 _. . Appendix A1.1.4 Get_rate_frompdb.sh #!/bin/sh j =0 until [ $j = 72 do j= echo "$j+l" bc get-rate_from_pdb 33 a$j.pdb echo "\r" done echo A1.1.5 \007" Getratefirmpdb.c The program calculates the F-rates for purines. In order to obtain the F-rates from pyrimidines, the CB and H 8 have to be replaced by Q and H. /* get_ratefromypdb.c Calculates theta from given pdb file ./ #include "stdio.h" #include "math.h" int int char float float float int char dum2,dum5; number; duml,dum4; dum9,dumlO; test_x,test_y,test_z; testl; restest,maxno; atoml[8] ,atom2[8],atom3[8],atom4 [8],atom5 [8] ,atom6[8],atom7[8] ,atom8 [8],atom9 [9]; float N_x,N_y,N_z,NHl_x,NHl_y,NHlz,NH8_x,NH8_y,NH8_z,Clx,Cly,Cl_z,Hl_x,Hly,Hl_z float float float float float float float float test_neu; atom3_x,atom3_y,atom3_z,atom4_x,atom4_y,atom4_z; Sll_x,Sll_y,Sll_z,S22_x,S22_y,S22_z; C2H2_x,C2H2_y,C2H2_z,betrag_C2H2,H2_x,H2_y,H2_z; C8H8_x,C8H8_y,C8H8_z,betrag_NH8,H8_x,H8_y,H8_z; ClHl_x,ClHl_y,ClHl_ z,betrag_NHl; Nx_x,Nx_y,Nx_z,betrag_Nx,Ny_x,Ny_y,Ny_z,Nz_z,Nz_x,Nz_y,betrag_Ny,betrag_Nz; sigma_llx,sigmally,sigmall z,sigma_22 x,sigma_22_y,sigma_22_z,sigma_33_x, sigma_33_y,sigma 33_z; float ein _xbetr,ein_y_betr,einzbetr; float betr sigmall,betr_sigma_22,betr sigma_33; float betragl,betrag2,betrag3; float cos2_THETA,cos2_THETAy; float gammac,gamma_c_cl,gammac c2; float s_ll,s_22,s_33,C; float theta; float invcostx, winkel; char atomtype[8]; FILE *fin, *fout; main (argc,argv) int argc; char *argv[]; if (argc (argc != != 3) 3) if 189 Appendix {printf("\n\nget ilratefrom_pdb: printf("USAGE: get_lratefrompdb exit(l); } wrong number of arguments\n\n"); maxNoofAtomsinPDB file.pdb \n\n"); atoml[0]='P'; atoml [1]='19'; atom5 0] = 'H'; atom5[1]='1'; atom5[2] ='\'; atom9[0] = 'H'; atom9[1] =' 8'; sscanf(argv[l] ,"%d",&maxno); s 11= -150; s 22= -199; s_33= -291; C= 1.6988888; /* C= 0.0326999;*/ if ((fin=fopen(argv[2] , "r"))==NULL) { printf("ERROR opening file %s !\n",argv[2]); exit(l); } number=l; fseek(fin,0,0); while (number!=maxno) { fscanf(fin,"%s %d %s %s %d %f %f %f %f %f",&duml,&number,atomtype, \ &dum4,&restest,&testx,&test_y,&test_z,&dum9,&dumlO); if (strcmp(&atomtype[0] ,&atoml[0] )==0){ if (restest==l) { Nx=testx; N y=test_y; N_z=testz; } } number= 1; fseek(fin, 0,0) while (number<=maxno) { fscanf(fin,"%s %d %s %s %d %f %f %f %f %f",&duml,&number,atomtype, \ &dum4,&restest,&testx,&test_y,&test_z,&dum9,&dumlO); if (strcmp(&atomtype 0] , &atom5[0] ) ==0){ if (restest==l) { Hl_x=test_x; Hl_y=test_y; Hlz=testz; } } number= 1; fseek(fin,0,0); while (number<=maxno){ fscanf(fin,"%s %d %s %s %d %f %f %f %f %f",&duml,&number,atomtype, &dum4,&restest,&test_x, &test y,&test_z,&dum9,&dumlO0); if (strcmp(&atomtype[0] , &atom9[0] ) ==0) { if (restest==l) { H8 x=testx; H8_y=test_y; H8_z=testz; I~~~~ /* printf("\n\n"); 190 \ Appendix printf("Koordinaten printf("Koordinaten printf("Koordinaten von Atoml(%s): %.3f %.3f %.3f\n", atoml,N_x,N_y,N_z); von Atoml(%s): %.3f %.3f %.3f\n", atom5,Hl_x,Hl_y,Hl_z); von Atoml(%s): %.3f %.3f %.3f\n", atom9,H8_x,H8_y,HS_z); */ NH8_x = Nx - H8_x; NH8_y = N y - H8_y; NH8_z = N_z - H8_z; betrag_NH8= sqrt(pow(NH8_x,2)+pow(NH8_y,2)+pow(NH8_z,2)); NH1x= Nx - Hl_x; NH1_y = N_y - Hl_y; NHl_z = Nz - Hl_z; betrag_NHl= sqrt(pow(NH1_x,2)+pow(NHiy,2)+pow(NHlz,2)); cos2_THETA = ((NH1_x * NH8_x) + (NHl_y * NH8_y) *betrag_NH8); + (NHi_z * NH8_z))/(betragNHl gammac= C * ( (3 * cos2_THETA* cos2_THETA- 1)); winkel= acos (cos2_THETA)*180 printf("%9.3f /M_PI; %9.3f %9.3f"',cos2_THETA, gamma_c, winkel) ; fclose(fin); Coordinate file independent r-rate calculation A1.1.6 Cross-correlated relaxation rates were calculated by Gprogramms using the CS-tensor values and orientations given in Table A1. A1.1.6.1 r(HC,N) F(HCN) for adenine in the 14-nt RNA at 600MHz. /*calculation of HC,N CCRR in Adenine at 600MHz*/ #include #include #define #define #define stdio.h> <math.h> gammalH 26.7519e7 gammal3C 6.728e7 Hq 1.0546e-34 #define m /* gyromag. ratio 1H [sec* A* kg-1] */ /* gyromag. ratio 13C [sec* A* kg-1] */ /* Planck's h/2pi [J*sec] */ 0.9999995e-7 /* permeability of vacuum/4/pi [m*kg*sec-2*A-2] */ /* bond angle taken from cns2.0 force field for C3'-endo:*/ char s1[80]; int i,j,n,m,l; double alpha,beta,beta2,angleO,rch,rco,rop,rcn, s1Il,s22,s33, x_h,y_h,zh, x_ 3 3,y_33,z_33, x_22,y_22,z_22, xll,yll,z_11, x_hp,y_hp,z_hp, s33_length,s22_length, s11_length,hc_length, x_dotl,x_dot2,x_dot3, 191 Appendix costx,costy,costz,invcostx,invcosty, cosx_out,cosy out,cosz_out, thetal, theta2, ftheta, factor,angle_factor, ni,gammah,tauc,S,omegalSN, al,a2,c, rate,rateh8c8, cosx,cosy,cosz, x_h8c8,y_h8c8,zh8c8,h8c8_length, x_dot_h8c8,y_doth8c8,z_dot_h8c8, costx_h8c8,costyh8c8,costz_h8c8, fthetah8c8; main () { alpha = 180-108.7; /*angle between CH-vector and CN bond */ rch=1.09e-10; rcn=l.5e-10; omegal5N=2*M_PI*l.Oe6*60.808; al = -4*(mO*Hq*gammalH*gammal3C*omegal5N)/15; a2 = rch*rch*rch; S=1; /* order paramete r square */ tauc=1.9e-9; sll=-148; s22=-198; s33=-281; /*all vectors are calculated from N as the origin of the coordinate system x-axis is along NCl'-bond, z-axis orthogonal to base plane */ /*orientation of H8C8 */ x_h8c8=cos(71.33*M PI/180.0); y_h8c8=-sin(71.33*M_PI/180); z_h8c8=0; h8c8_length=sqrt(x_h8c8*xh8c8+y_h8c8*y_h8c8+z_h8c8*z_h8c8); /* orientation of sigmall */ x ll=cos(3.96*M PI/180.0); y_ll=-sin(3.96*M_PI/180.0); z_11=0; sll_length=sqrt(xll*xll+y_ll*yll+zll*z_ll); /* orientation of sigma22 */ x_22=cos(93.96*M_PI/180.0); y_22=-sin(93.96*M_PI/180.0); z_22=0; s22_length=sqrt(x_22*x_22+y_22*y_22+z_22*z_22); /* orientation of sigma33 */ x_33=0; y_33=0; z_33=1; s33_length=l; /* calculation of G(H8C8,N1) */ xdoth8c8=x h8c8*x ll+yh8c8*y_ll+z_h8c8*z_11; 192 Appendix y-dot h8c8=x_h8c8*x_22+y_h8c8*y_22+z_h8c8*z22; z_dot_h8c8=x_h8c8*x_33+y_h8c8*y_33+z_h8c8*z_33; costx_h8c8=(x_dot_h8c8/(h8c8_length*sll_length)); costy_h8c8=(y_doth8c8/(h8c8_length*s22 length)); costz_h8c8=(z_dot_h8c8/(h8c8_length*s33_length)); fthetah8c8=0.5*(sll*le-6*(3*costxh8c8*costx h8c8-l)+s22*le6*(3*costy_h8c8*costyh8c8-1)+s33*1e-6*(3*costz_h8c8*costz_h8c8-1)); rate_h8c8=(al*ftheta_h8c8*tauc)/a2; /* calculation of G(Hl'Cl',N9) */ for(j=0;j<360;j++){ angleo=(double)(j); /*definition of chi*/ beta2=angleO-240; /*orientation of the Hl'Cl'-vector*/ xh=rch*cos(alpha*MPI/180.0); /* x-position is fixed */ yh=rch*sin(alpha*MPI/180.0)*cos(beta2*M_PI/180.0); z_h=rch*sin(alpha*MPI/180.0)*sin(beta2*M_PI/180.0); hclength=sqrt((x_h*xh)+(y_h*y_h)+(z_h*z_h)); /*angle between sigmacomponents and Cl'Hl' */ xdotl=xh*xll+y_h*y_ll+z_h*z_11; x_dot2=x_h*x_22+y_h*y_22+zh*z_22; x_dot3=x_h*x_33+y_h*y_33+z_h*z_33; /* projection angle */ costx=(x_dotl/(hc length*sll_length)); costy=(xdot2/(hc length*s22_length)); costz=(x_dot3/(hclength*s33_length)); /* relaxation rate */ ftheta=0.5*(sll*1.Oe-6*(3*costx*costx-l)+s22*1.0e-6*(3*costy*costy-l)+s33*1.0Oe6*(3*costz*costz-1)); printf("%d %e %e \n",j,rate, rate_h8c8); A1.1.6.2 (HN,C) for the base moiety /*calculation of the unwanted HN,C CCRR in Adenine at 600MHz*/ #include <stdio.h> #include <math.h> #define gammalH 26.7519e7 /* gyromag. ratio H [sec* A* kg-l */ #define gammal5N -2.75e7 /* gyromag. ratio 15N [sec* A* kg-l */ #define gammal3C 6.728e7 /* gyromag. ratio 13C [sec* A* kg-l */ #define Hq 1.0546e-34 /* Planck's h/2pi [J*sec] */ #define m 0.9999995e-7 /*permeability of vacuum/4/pi [m*kg*sec-2*A-2]*/ /* bond angle taken from cns2.0 force field for C3'-endo:*/ 193 Appendix char int double sl ([80]; i,j,n,m,1; alpha,rch, al, a2, sll,s22,s33, thetall,theta22, ftheta, theta33, ni,gammah,tauc,S,omegal5N, ratehnc; main () { rch=2.15e-10; omegal5N=2*MPI*1.0e6*70.947; al -4*(mO*Hq*gammalH*gammal3C*omegal5N)/15; a2 = rch*rch*rch; /* order parameter S=1; tauc=1.9e-9; /*---------------------------------- ADENINE square */ -------------------------------------- - ,/ s11=216; s22=136; s33=61; thetall=cos(4.8*M_PI/180.0); theta22=cos(94.8*M_PI/180.0); theta33=cos(90*M_PI/180.0); ftheta=0.5*(sll*le-6*(3*thetall*thetall-1) 1)+s33*1e-6*(3*theta33*theta33-1)); +s22*1e-6*(3*theta22*theta22- ratehnc=(al*ftheta*tauc)/a2; printf("G(HNC) for adenine= "); printf(" %e \n",rate_hnc); %e %e \n", sl, s22, s33); printf("%e printf("%e %e %e \n", 3*thetall*thetall-1, 3*theta33*theta33-1); printf(" %e \n",ftheta); printf(" %e %e \n",al, a2); /*---------------------------------- 3*theta22*theta22-1, GUANINE -------------------------------------- sll=214; s22=141; s33=59; thetall=cos(3.8*M_PI/180.0); theta22=cos(93.8*M_PI/180.0); theta33=cos(90*M_PI/180.0); ftheta=0.5*(sll*le-6*(3*thetall*thetall-1) 1)+s33*1e-6*(3*theta33*theta33-1)); +s22*1e-6*(3*theta22*theta22- ratehnc=(al*ftheta*tauc)/a2; printf("G(HCN) for guanine= ") printf(" %e \n",ratehnc); %e %e \n", 3*thetall*thetall-1, printf("%e 3*theta33*theta33-1); printf(" %e \n",ftheta); 194 - 3*theta22*theta22-1, Appendix /*---------------------------------- CYTOSINE ------------------------------------- */ -- s11=241; s22=152; s33=35; thetall=cos(4.7*M_PI/180.0); theta22=cos(94.7*MPI/180.0); theta33=cos(90*M_PI/180.0); ftheta=0.5*(sll*le-6*(3*thetall*thetall-1)+s22*1e-6*(3*theta22*theta221)+s33*1e-6*(3*theta33*theta33-1)); ratehnc=(al*ftheta*tauc)/a2; printf("G(HCN) for cytosine= "); printf(" %e \n",rate_hnc); printf("%%e e %e \n", 3*thetall*thetall-1, 3*theta33*theta33-1); printf(" %e \n",ftheta); /*---------------------------------- 3*theta22*theta22-1, THYMINE -------------------------------------- s11=238; s22=128; s33=42; thetall=cos(5.7*M_PI/180.0); theta22=cos(95.7*M_PI/180.0); theta33=cos(90*M_PI/180.0); ftheta=0.5*(sll*le-6*(3*thetall*thetall-l)+s22*1e-6*(3*theta22*theta221)+s33*1e-6*(3*theta33*theta33-1)); ratehnc=(al*ftheta*tauc)/a2; printf('"G(HCN) for thymine= ); printf(" %e \n",ratehnc); printf("%%e e %e \n", 3*thetall*thetall-1, 3*theta33*theta33-1); printf(" %e \n",ftheta); } 3*theta22*theta22-1, /*calculation of the unwanted HN,C CCRR in Adenine at 600MHz*/ #include <stdio.h> #include <math.h> #define gammalH 26.7519e7 /* gyromag. ratio 1H [sec* A* kg-1] */ #define gammal5N -2.75e7 /* gyromag. ratio 15N [sec* A* kg-1] */ #define gammal3C 6.728e7 /* gyromag. ratio 13C [sec* A* kg-1] */ #define Hq 1.0546e-34 /* Planck's h/2pi [J*sec] */ #define m 0.9999995e-7 /* permeability of vacuum/4/pi m*kg*sec-2*A-2] */ A1.2 References 1. Fiala, R; Czernek J.;Sldenar, V. (2000). Transverse relaxation optimized triple-resonance 2. NMR experiments for nucleic acids.JBiwr NMR, 16,291-302. Stueber, D. and Grant, D. M. (2002). (13)C and (15)N chemical shift tensors in adenosine, guanosine dihydrate, 2'-deoxythymidine, and cytidine.JAmbemnSaoc, 124, 10539-10551. 195 Appendix CHAPTER 3: RNA Tetraloop Dynamics A2 A2.1 Pulse sequences A2.1.1 R1 ;hsqctletf2gpsi ;avance-version (03/01/27) ;2D H-1/X correlation via double inept transfer using sensitivity improvement ;for measuring C-13 T1 relaxation times ;phase sensitive using Echo/Antiecho-TPPI gradient selection ;with decoupling during acquisition ;using f3 - channel ;using flip-back pulse ;(use parameterset HSQCT1ETF3GPSI) prosol relations=<triple> d26 UNBLKGRAD (pl ph2) #include <Avance.incl> #include <Grad.incl> #include <Delay.incl> "p2=pl*2" 4u plO:fl (pll:spl phl:r):fl 4u p16:gpl d16 pll:fl "p4=p3*2" (p3 ph3):f2 d25 (center (p2 phl) (p4 phl):f2 d25 pll9:fl (p3 ph2):f2 "dO=3u" "dll=30m" "d24=ls/(cnst4*cnstll)" (p26 ph2):fl TAU cpdsl:fl phl 4u do:fl (p26 ph7):fl 4u p16:gp4 d16 pll:fl "d25=ls/(cnst4*cnstl2)" "d26=ls/(cnst4*4)" "DELTA2=p19+d16+8u" "DELTA3=d25-p19-d16-8u-p8" # (p3 ph8):f2 4u ifdefLABELCN p19:gp2*-l*EA "DELTAl=d25-p19-d16-larger(p2,p8)d0*2" # else "DELTAl=d25-p19-d16-p2-dO*2" # endif /*LABEL_CN*/ d16 plO:f2 (pB:spl3 phl):f2 4u DELTA3 p2:f2 (p4 ph6):f2 dO (center (p2 ph9) (p8:spl3 phl):f2 # else (p2 ph9) # endif /*LABEL_CN*/ 1 ze dll pll2:f2 stO 2 6m do:f2 3 3m 4 dll 5 dll "d7=vd" "TAU=d7-p26*2-p16-d16-8u" dl (pl phl) dO p19:gp2*EA d16 DELTA1 (center (pl phl) d24 (center (p2 phl) d26 p2:f2 (center (p2 phl) ifdefLABELCN # aqseq 312 (p4 phl) :f2 ) 196 (p3 ph4):f2 ) (p4 phl):f2 ) Appendix d24 (center (pl ph2) (p3 ph5):f2 d26 (center (p2 phl) (p4 phl):f2 d26 (pl phi) DELTA2 (p2 phi) 4u pl9:gp3 d16 pll2:f2 4u BLKGRAD ) dll mc #0 to 5 F2EA(igrad EA & ip5*2, idO & ip6*2 & ip8*2 & ip3l*2) ) exit phO=0 phl=0 ph2=1 ph3=0 0 0 0 2 2 2 2 ph4=0 0 2 2 ph5=3 3 1 1 ph6=0 ph7=3 ph8=l 3 ph9=0 0 2 2 ph31=0 2 2 0 2 0 0 2 goscnp ph31 cpd2:f2 3m do:f2 3m st ivd lo to 3 times nbl 3m ipp3 ipp4 ipp5 ipp8 ipp9 ipp31 lo to 4 times ns ;d7 : delay for inversion recovery [30 msec] ;dll: delay for disk I/O ;d16: delay for homospoil/gradient recovery ;d24: 1/(4J)YH for YH ; 1/(BJ)YH for all multiplicities ;d25: 1/(4J)YH for YH ; 1/(8J)YH for all multiplicities ;d26: 1/(4J(YH)) ;cnst4: = J(YH) ;cnstll: for multiplicity selection = 4 for NH, 8 for all multiplicities ;cnstl2: for multiplicity selection = 4 for NH, 8 for all multiplicities ;in0: 1/(2 * SW(X)) = DW(X) ;ndO: 2 ;NS: 1 * n ;DS: >= 16 ;tdl: number of experiments ;FnMODE: echo-antiecho ;cpdsl: decoupling according to sequence defined by cpdprgl ;cpd3: decoupling according to sequence defined by cpdprg3 ;pcpdl: fl channel - 90 degree pulse for decoupling sequence ;pcpd3: f2 channel - 90 degree pulse for decoupling sequence ;use gradient ratio: gp 1 : gp 2 : gp 3 : gp 4 50 : 80 : 16.2 : 30 for N-15 ;for z-only gradients: ;gpzl: 50% ;gpz2: 80% ;gpz3: 16.2% ;gpz4: 30% ;preprocessor-flags-start ;LABEL_CN: for C-13 and N-15 labeled samples start experiment with ; ~ option -DLABEL CN (eda: ZGOPTNS) ;preprocessor-flags-end ;$Id: hsqctletf2gpsi,v 1.1.2.2 2003/01/31 11:45:02 ber Exp $ 197 Appendix A2.1.2 Rlp ;hsqctretf2gpsi.t5 ;avance-version (03/04/25) ;2D H-1/X correlation via double inept transfer using sensitivity improvement ;for measuring C-13 Trho relaxation times ;phase sensitive using Echo/Antiecho-TPPI gradient selection ;with decoupling during acquisition ;using f3 - channel ;using flip-back pulse ;(use parameterset HSQCTRETF3GPSI) ;K.T. Dayie & G. Wagner, J. Magn. Reson. A 111, 121-126 (1994) ;F.A.A. Mulder, R.A. de Graaf, R. Kaptein & R. Boelens, ; J. Magn. Reson. 131, 351-357 (1998) . Millet, D.A. Torchia & ;D.M. Korzhnev, N.R. Skrynnikov, ; L.E.Kay, J. Am. Chem. Soc. 124, 10743 (2002) (pl phl) d26 p12:f2 (center (p2 phl) (p4 phl):f2 d26 UNBLKGRAD (pl ph2) 4u p16:gpl d16 pll:fl (p3 ph3):f2 d25 (center (p2 phl) (p4 phl):f2 d25 pll9:fl (p3 phll):f2 ;phaseOnTcu prosol relations=<triple> #include <Avance.incl> #include <Grad.incl> #include <Delay.incl> "Ip2=pl*2" "p4=p3*2" "p22=p2 l* 2 " "dO=3u" "dll=30m" "dl2=20u" "d24=ls/(cnst4*cnstll)" "d25=ls/(cnst4*cnstl2)" "d26=ls/(cnst4*4)" p16 :gp5 d16 plO:f2 4u fq=cnst30(sfo hz):f2 (p 2 9:spl9 phl):f2 4u 4u p125:f2 4u cpds8:f2 ph8 "cnst29=0" "DELTA2=p19+dl6+8u" "DELTA3=d25-p19-d16 -p8 - 8u" "DELTA4=d24-p19-d16" "DELTA5=d26-pl6-dl6" # "p30=random(p31,cnst31)" 6 (p30 phlOA) :fl "d31=d31-p30" "p30=random(p31,cnst31)" if "d31 < p30" { "p30=d31" if "p30 < 3u" { "p30=3u" } goto 7 } else { goto 6 ifdef LABEL CN "DELTAl=d25-pl9-dl6-larger(p2,p8) d0*2-4u" else # "IDELTAl=d25-pl9-dl6-p2-dO*2 # endif /*LABEL_CN*/ aqseq 312 1 ze dll p112:f2 stO 2 6m do:f2 3 3m 4 dll 5 dll p125:f2 7 (p30 phlO ^) :fl "d31=vd" dl fq=cnst29(sfo hz):f2 4u pll:fl 4u do:f2 4u plO:f2 (p29:sp20 phl):f2 4u 4u fq=cnst29(sfo hz):f2 30m p16 :gp4 198 ) ) Appendix dl6 (pl phi) DELTA2 (p2 phi) 4u p19 :gp3 d16 pll2:f2 4u BLKGRAD goscnp ph31 cpd2:f2 d16 p12:f2 (p3 phl2)::f2 4u 4u p10:f2 (p8:spl3 phl):f2 p19 :gp2*-]*EA d16 DELTA3 pll:fl p2:f2 (p4 ph6):f2 dO 4u plO:f2 p3:f3 # ifdefLABELCN (center (p2 ph7) # 3m do:f2 3m st ivd lo to 3 times nbl 3m ipp3 ipp4 ipp5 ipp6 ipp7 ipp31 lo to 4 times ns (p8:spl3 phl):f2 (p22 phl):f3) else dll mc #0 to 5 F1QF() F2EA(igrad EA & ip5*2 , id0 & ipl2*2 & ip31*2) exit (p2 ph7) # endif /*LABEL_CN*/ dO p19 :gp2*EA d16 p2:f2 DELTA1 (center p19 :gp6 d16 DELTA4 (center DELTA4 p19:gp6 d16 (center p16:gp7 d16 DELTA5 (center DELTA5 p16:gp7 (pl phl) (p3 ph4):f2 ) phO=0 phl=0 ph2=1 ph3=0 2 (p2 phl) (p4 phl):f2 ) ph4=0 ph5=3 ph6=0 ph7=0 (pl ph2) (p3 ph5):f2 ) (p:2phl) (p4 phl):f2 ) ph8=0 ph9=2 phlO=l 3 phll=l phl2=1 ph31=0 0 3 0 0 0 3 1 0 0 3 1 0 2 1 2 2 2 1 2 2 2 1 3 2 2 1 3 2 2 2 0 2 0 0 2 ;d20: wanted Trho delay ;d21: maximum Trho delay in series ;d24: 1/(4J)YH for YH ; 1/(8J)YH for all multiplicities ;d25: 1/(4J)YH for YH ; 1/(8J)YH for all multiplicities ;d26: 1/(4J(YH)) ;cnst4: = J(YH) ;cnstll: for multiplicity selection = 4 for NH, 8 for all mu:Itiplicities ;cnstl2: for multiplicity selection = 4 for NH, 8 for all mu.ltiplicities ;cnst28: on resonance frequency f2 [in ppm] f2 [in ppm] ;cnst29: off resonance frequency ;cnst30: difference in frequency [in Hz] ;14: loop for Trho delay ;15: loop for compensation of heating effects = 14(max) - 14 (current) ;in0: 1/(2 * SW(X)) = DW(X) ;nd0: 2 ;NS: 1 * n ;DS: >= 16 ;tdl: number of experiments ;FnMODE: echo-antiecho ;cpd3: decoupling according to sequence defined by cpdprg3 ;pcpd3: f2 channel - 90 degree pulse for decoupling sequence ;use gradient ratio: gp 30 : 1 : gp 2 : gp 3 80 : 16.2 for N-15 ;for z-only gradients: 199 Appendix ;gpzl: ;gpz2: ;gpz3: ;gpz4: ;gpz5: ;gpz6: ;gpz7: 30% 80% 16.2% 50% -40% 5% -2% ;use gradient files: ;gpnaml: SINE.100 ;gpnam2: SINE.100 ;gpnam3: SINE.100 ;gpnam4: SINE.100 ;preprocessor-flags-start ;LABELCN: for C-13 and N-15 labeled samples start experiment with ; ~ option -DLABEL_CN (eda: ZGOPTNS) ;preprocessor-flags-end ;$Id: hsqctretf2gpsi,v 1.1.2.1 2002/07/16 12:59:36 ber Exp $ 200 Appendix A2.1.3 3C HetnOe ;invinoef2gpsi ;avance-version ;2D H-1/X correlation via double inept transfer ;using sensitivity improvement ;for measuring Hl-C13 NOEs ;phase sensitive using Echo/Antiecho-TPPI gradient selection ;recording NOE and NONOE interleaved #include <Avance. incl> #include <Grad.incl> #include <Delay.incl> p16 :gp2*-l*EA dl6 DELTA3 (p4 ph6):f2 4u dO plO:f2 p3:f3 (CEN_HC2 p2 ph9):fl 22 phl):f3 (CENCN1 p (p14:sp3 phl):f2 dO 4u p12:f2 "pO=pl* 4 /3" "p2=pl*2" "p4=p3*2" "dO=3u" "dll=30m" "d12=20u" "d24=ls/(cnst4*cnstll)" "d25=ls/(cnst4*cnstl2)" "d26=ls/(cnst4*4)" p16:gp2*EA d16 DELTA1 (CEN_HN1pl phl) (p3 ph4):f2 d24 4 (CENHN2 p2 phl) (p phl):f2 d24 (CEN_HN1 pl ph2) (p3 ph5):f2 d26 (CENHN2 p2 phl) (p4 phl) :f2 d26 (pl phl) DELTA2 (p2 phl) 4u p16:gp3 d16 pll2:f2 4u BLKGRAD go=2 ph31 cpd2:f2 dll do:f2 wr #0 if #0 zd "DELTAl=d25-p16-d16-p14-dO*2-4u" "DELTA2=p6+dl6+8u" "DELTA3=d25-p16-d16- 8u-p14" "CENHC2=(p14-p2)/2" "CEN HNi=(p3-pl)/2" "CEN HN2=(p4-p2)/2" "CENCNl=(p14-p22)/2" "10=0" "13= (tdl/4) "14=dl/(pO*4/3+5m) 1 ze dll pl2:f2 2 dll do:f2 6m 3 3m 4 dll 12m 5 d12 6m ip5*2 igrad EA lo to 3 times 2 3m iu0 lo to 4 times 2 if "10 %2 .= 1" goto 100 dll idO ip6*2 6m ip8*2 6m ip31*2 lo to 5 times 13 6 (p0 phl) 5m lo to 6 times 14 4u goto 101 exit phl=0 ph2=1 ph4=0 0 2 2 ph5=3 3 1 1 ph6=0 ph7=3 ph8=1 3 ph9=0 0 2 2 ph31=0 2 2 0 100 dl 101 50u UNBLKGRAD (pl phi) 4u p16:gpl d16 pl2:f2 (p3 ph8):f2 4u (pl4:sp3 phl):f2 201 Appendix A2.2 Extraction of peak intensities The spectra were transferred to felix (msi) and the peak intensities were extracted from the picked peaks by a grid search using the macro autopkhpos.mac A2.2.1 Autopkhpos.mac c** autopkhpos.mac - Oz TSRI Jan 1997 c** get peakheights for only positive peaks c** use for analysis of T2 and Tlrho data def fitm 1 ; first item def litm 14 ; last peak numer def smxfil tlr ; dataname for count 1 10 ; 1st and last number of datasets mat &smxfil&count.mat ty opening &smxfil&count.mat for ii &fitm &litm dba element load xpk:peaks.&ii.cenl poil dba element load xpk:peaks.&ii.cen2 poi2 def wdthl 4 ;gridsearch 6 points def wdth2 4 ;gridsearch 6 point def pkht 0.0 def temp 0.0 def maxp 0.0 for nrow 0 &wdth2 eva row (&poi2+&nrow-(&wdth2)/2) loa 0 &row for ncol 0 &wdthl eva col (&poil+&ncol-(&wdthl)/2) gv &col temp if &temp t &maxp againa eva maxp &temp againa: next next ty &ii &maxp $ dba element store vol:volumes.&ii.vol&count &maxp esc out if &out ne 0 escape next cmx next escape: ex &return end 202 Appendix A3 CHAPTER 4: Structure of the TCR 4-chain A3.1 Assignment of free TGR 4 at 278K 298K 278K Residue N HN Ca 40.45 55.30 52.36 53.14 59.19 53.45 55.00 54.87 53.24 55.74 50.03 51.38 48.07 60.38 49.83 55.31 52.71 53.45 42.69 53.24 50.86 53.66 53.14 55.31 50.55 54.17 54.07 50.55 52.88 42.48 53.35 53.45 53.76 54.48 55.00 51.48 60.59 52.80 52.00 53.97 54.07 53.66 42.59 1 2 3 4 5 6 7 8 9 10 11 12 13 115.17 124.09 122.75 121.92 125.11 121.71 117.99 122.90 117.47 125.27 118.00 124.59 8.50 8.27 8.23 7.99 8.17 8.15 8.05 8.25 8.24 8.24 7.93 7.80 123.34 118.74 122.15 121.33 109.92 119.12 118.89 120.15 121.79 119.62 119.90 120.81 121.13 117.84 121.41 108.27 8.19 7.89 7.94 8.16 8.32 8.03 8.32 8.14 7.96 7.91 8.00 8.20 7.93 8.05 7.97 8.17 7.86 8.27 8.39 8.18 7.87 8.20 7.82 8.00 7.87 8.16 8.10 7.87 8.17 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 120.07 122.60 121.57 120.80 119.63 121.71 119.84 122.37 120.15 122.38 119.56 120.13 109.23 203 CB C, 60.94 39.55 27.89 30.15 30.27 36.94 60.83 28.11 60.83 16.12 38.30 15.44 29.47 16.23 35.93 26.98 26.42 166.85 178.01 172.70 174.87 175.38 175.16 176.02 178.96 174.32 177.65 172.31 175.74 26.76 36.04 26.53 39.44 35.93 35.81 27.21 36.04 39.32 28.00 27.89 27.44 27.28 35.93 38.55 29.59 38.87 38.42 29.47 27.32 27.66 cI 173.69 171.73 175.41 176.05 173.75 178.10 175.02 176.50 175.02 172.50 175.48 176.38 174.89 172.39 173.59 171.01 178.79 174.35 174.28 174.20 174.52 175.83 173.78 173.78 172.20 173.14 172.45 173.44 173.31 Appendix 44 45 119.63 122.87 7.92 8.26 52.93 49.93 28.34 37.96 179.26 175.08 46 -- -- 60.83 29.36 -- 47 48 49 50 51 119.59 120.53 109.72 108.04 121.26 8.34 8.10 8.29 8.07 7.92 53.86 52.93 42.59 42.38 51.69 26.98 35.81 --29.47 172.75 173.14 173.03 177.49 179.32 52 -- -- 59.93 -- -- 53 54 55 56 121.79 122.83 123.34 121.11 8.35 8.28 8.34 8.45 53.14 53.04 53.40 48.28 28.11 28.11 30.49 35.81 173.52 174.47 174.85 174.91 57 -- -- 60.94 29.25 -- 58 59 60 61 62 63 64 65 66 67 68 69 70 71 72 73 74 75 76 77 78 79 80 81 82 83 84 85 86 87 88 89 90 91 92 93 94 95 96 118.14 121.27 109.60 120.81 119.86 120.00 120.87 121.34 119.93 121.72 120.14 121.05 120.00 123.85 119.40 123.71 118.82 116.95 122.45 120.44 111.84 119.27 121.35 109.20 120.46 121.94 121.94 122.00 109.76 120.23 109.54 118.29 120.31 108.42 120.81 120.51 122.37 108.56 120.75 8.16 7.93 8.23 7.74 8.02 8.06 8.18 7.97 7.99 8.02 8.14 7.97 8.08 7.92 8.07 7.98 7.92 7.79 8.18 7.86 8.26 7.98 8.24 8.17 8.13 8.25 8.21 8.26 8.29 8.15 8.35 8.23 8.21 8.18 7.81 8.10 8.10 7.60 7.94 53.35 53.86 42.69 52.31 55.31 50.46 26.08 26.98 -39.59 36.04 36.04 172.97 174.88 173.18 178.83 172.57 175.63 176.51 176.33 171.52 174.28 173.43 173.75 172.53 174.08 170.73 173.89 171.67 175.05 178.48 173.58 172.89 177.96 173.64 172.61 178.60 173.81 174.26 174.53 173.47 179.13 172.48 178.64 177.49 171.01 178.66 172.48 175.22 175.16 179.27 . 52.80 53.24 54.18 51.59 53.97 53.24 50.29 54.17 50.03 55.41 55.52 53.86 58.72 42.59 53.06 53.55 42.59 53.66 53.49 53.40 53.45 42.59 53.66 42.48 53.32 51.76 42.59 52.41 55.31 52.93 42.28 52.41 204 39.14 26.30 30.15 38.19 29.81 29.59 16.23 27.32 16.23 35.81 60.94 27.32 35.70 -29.93 29.81 -27.32 27.90 27.78 27.89 -30.15 -26.76 38.30 -39.55 29.81 26.76 -39.89 Appendix 97 98 99 100 101 102 103 104 105 106 107 108 109 110 111 112 116.50 115.47 125.63 113.63 123.12 120.59 113.78 122.23 121.87 123.27 117.25 116.96 119.92 120.68 125.05 122.82 8.28 8.01 8.05 7.96 8.17 8.17 7.77 8.03 8.16 7.95 7.72 7.70 7.94 8.13 8.09 8.06 55.52 59.14 50.03 59.35 54.07 52.10 59.66 56.35 54.90 51.24 52.93 53.14 53.06 52.97 49.52 50.04 60.94 66.49 16.49 66.80 30.15 37.96 66.72 35.81 37.96 37.85 39.21 25.96 29.81 26.53 16.45 38.87 171.59 176.88 178.10 170.93 177.24 174.22 173.67 177.82 174.64 173.81 169.79 171.78 177.84 174.49 176.13 172.38 7.80 60.15 54.53 28.91 174.75 113 114 115 125.86 Table A2:Assigvrm ff A3.2 Assignment of free TCR 4 TCR at 278K at 317K 310K Residue N HN 124.03 122.18 120.71 124.26 121.14 8.54 8.52 8.16 8.41 8.35 122.87 8.55 125.19 118.19 124.29 8.50 8.29 8.09 50.53 51.90 48.37 123.06 117.97 121.46 120.96 109.59 119.30 118.87 120.06 121.87 119.30 119.64 120.70 120.97 8.43 8.09 8.27 8.45 8.58 8.39 8.61 8.46 8.28 8.18 8.36 8.54 8.26 50.44 55.65 53.45 54.19 43.16 53.80 51.34 54.01 53.24 55.87 51.21 54.83 53.37 CB C, 4.26 3.99 4.13 169.36 172.13 171.05 170.72 170.93 1 2 3 4 5 6 7 53.11 53.71 59.78 54.06 55.22 8 9 171.24 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 4.46 169.50 172.28 170.53 4.26 - 205 4.57 4.19 4.16 4.21 4.55 4.17 4.15 5.06 4.54 4.08 4.17 171.81 172.65 170.83 170.64 171.55 169.33 170.94 170.85 172.16 170.71 170.27 171.72 Appendix 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 118.10 121.41 108.26 120.07 122.43 121.55 120.63 119.48 121.44 119.01 122.87 120.02 121.48 119.63 120.25 109.07 119.70 122.60 8.43 8.27 8.50 8.20 8.56 8.73 8.52 8.17 8.49 8.09 8.33 8.27 8.38 8.42 8.26 8.47 8.26 8.50 51.13 -43.12 53.67 54.06 54.62 54.53 55.61 52.20 60.69 53.50 52.33 54.75 54.49 54.27 43.08 53.58 50.48 4.19 3.83 4.27 4.18 4.14 4.11 -4.52 3.94 4.16 4.43 4.12 4.15 4.19 3.85 --- 172.27 170.25 172.92 169.05 171.26 171.34 171.44 171.22 170.59 171.50 171.51 172.44 171.86 172.19 171.72 171.82 168.85 170.81 -- 46 -- -- -- 4.27 172.15 47 48 49 50 51 121.07 120.23 109.35 108.06 121.22 8.58 8.41 8.58 8.39 8.21 54.53 53.58 43.33 42.86 51.90 -4.37 3.87 3.85 -- 172.24 171.95 171.91 169.71 168.83 52 -- -- -- 4.30 -- 53 54 55 56 121.44 122.18 122.85 120.87 8.60 8.50 8.58 8.70 53.76 4.21 54.06 48.98 4.21 -4.18 -- 171.84 171.24 171.00 170.95 57 -- -- -- 4.27 -- 58 59 60 61 62 63 118.01 120.96 109.32 120.95 119.48 119.82 8.48 8.26 8.52 8.07 8.28 8.39 53.93 54.87 43.20 53.15 55.69 51.21 4.21 4.15 3.82 4.17 4.14 -- 172.08 171.08 171.95 169.04 172.14 170.72 64 -- -- -- -- -- 65 66 67 68 69 70 71 72 73 74 75 76 77 78 79 80 121.29 119.79 121.56 119.97 120.74 119.85 123.71 119.06 123.45 118.38 116.49 122.32 119.96 111.33 119.44 121.22 8.28 8.32 8.32 8.48 8.29 8.41 8.26 8.39 8.26 8.19 8.16 8.52 8.16 8.54 8.31 8.51 53.32 53.71 54.87 52.46 54.44 53.54 50.78 54.66 50.35 55.95 56.04 54.66 59.53 43.12 53.45 54.40 4.18 4.18 4.12 4.48 4.16 4.30 171.36 4.09 --4.24 4.20 -3.84 4.34 4.21 171.66 172.59 171.29 171.62 171.57 172.08 -173.11 171.53 172.62 171.00 169.42 171.74 171.99 169.47 171.51 206 Appendix 81 82 83 84 85 86 87 88 109.06 120.57 121.71 121.60 121.78 109.59 120.38 109.47 -4.17 -- 43.08 54.44 54.01 53.88 54.01 43.12 54.10 42.95 8.48 8.48 8.55 8.49 8.52 8.59 8.43 8.63 -- -3.87 4.21 -- 172.12 169.17 171.62 171.32 171.17 171.67 168.87 172.14 89 -- -- -- -- -- 90 91 92 93 94 95 96 97 98 99 100 101 102 103 104 105 106 107 108 109 110 111 112 120.72 108.49 121.02 120.03 121.84 108.71 120.97 116.20 114.96 125.57 112.90 122.72 120.56 113.23 121.90 121.63 123.44 118.05 117.35 119.72 120.21 124.55 122.45 8.53 8.51 8.14 8.33 8.39 8.09 8.21 8.54 8.26 8.38 8.22 8.45 8.48 8.10 8.33 8.39 8.27 8.15 8.15 8.24 8.41 8.34 8.25 52.33 43.38 53.11 55.65 53.67 43.12 52.94 56.12 59.61 50.40 59.57 54.36 52.46 59.83 56.34 52.16 51.21 4.10 4.49 3.81 4.18 4.37 4.18 3.80 4.31 53.63 -49.92 50.61 -4.20 4.00 -- 171.71 169.53 169.19 172.19 170.85 171.07 168.92 172.62 169.95 169.35 172.87 169.70 171.26 169.47 169.49 170.81 171.39 173.39 172.70 170.02 171.14 170.33 172.11 113 114 --- --- --- -4.31 --- 115 125.53 8.01 55.09 -- 171.09 -- 4.32 4.37 4.30 -4.52 4.21 -4.41 --- -- Table A3: A ssigmrntqffie TCR (at310K A3.3 Assignment of TCR 4/LMPG at 3 10K ~/LMPG 310K Residue N HN 41.33 56.07 53.21 54.12 59.77 53.71 55.22 55.75 53.79 56.31 50.69 1 2 115.04 123.57 3 120.51 4 118.44 5 122.76 6 119.88 7 115.57 8 9 122.26 116.30 10 11 125.27 ~ ~~~~~~~~~~~~~~~~~., 8.58 8.42 8.20 7.74 7.91 8.17 8.01 8.44 8.32 8.32 207 CB C 61.97 40.34 28.53 30.68 31.17 37.69 62.05 28.61 61.72 16.97 115.04 123.57 120.51 118.44 122.76 119.88 115.57 122.26 116.30 125.27 I Appendix 12 13 117.28 123.91 8.10 7.86 51.67 48.71 38.85 15.98 117.28 123.91 - -- -- -- 15 16 17 18 19 20 21 22 23 122.40 117.20 120.69 119.97 108.88 119.52 118.18 119.99 120.69 8.33 7.87 8.04 8.25 8.39 8.28 8.34 8.34 8.18 50.95 56.24 54.40 54.50 43.69 54.79 52.21 55.10 55.02 16.81 36.13 26.96 26.80 -26.88 36.46 26.63 39.76 122.40 117.20 120.69 119.97 108.88 119.52 118.18 119.99 120.69 24 25 --- --- --- --- --- 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 118.98 118.35 116.92 120.14 107.26 119.52 121.18 120.44 119.41 118.79 121.09 118.62 121.05 119.42 120.60 119.34 119.88 108.83 119.59 122.69 8.20 7.85 8.00 8.06 8.32 8.00 8.22 8.54 8.35 7.92 8.24 7.92 8.04 8.05 8.14 8.19 8.09 8.31 8.06 8.35 55.12 53.29 51.26 53.56 43.44 53.98 54.21 54.96 54.79 55.71 52.52 61.00 53.55 52.70 54.67 54.62 54.30 43.17 53.40 50.14 26.94 39.82 36.04 39.84 118.98 118.35 116.92 120.14 107.26 119.52 121.18 120.44 119.41 118.79 121.09 118.62 121.05 119.42 120.60 119.34 119.88 108.83 119.59 122.69 -- 14 -- 28.20 28.28 27.54 27.46 36.46 38.68 30.02 39.68 38.85 30.26 28.20 28.37 -28.78 38.93 46 -- -- -- -- -- 47 48 49 50 51 118.90 119.40 109.10 108.11 121.40 8.51 8.13 8.30 8.21 8.11 54.76 53.27 43.35 43.00 51.99 27.54 --30.35 118.90 119.40 109.10 108.11 121.40 52 -- - -- -- -- 53 54 55 56 121.41 122.29 122.31 120.06 8.42 8.42 8.41 8.55 53.65 53.79 53.87 48.97 28.70 28.70 31.01 36.54 121.41 122.29 122.31 120.06 -- 57 -- -- -- -- -- 58 59 60 61 117.64 119.90 108.11 121.05 8.63 7.98 8.29 8.00 55.00 55.44 43.69 54.69 26.30 27.79 -40.01 117.64 119.90 108.11 121.05 -- -- -- -- 62 63 64 . . -. . . . . . 208 65 . . 66 67 68 69 . . . . . . . 70 .... . . . . . . . . . 71 72 122.40 122.04 73 -- . . . . . . . . . . . . . . . . . 8.08 8.04 -- 52.77 52.47 16.36 16.38 122.40 122.04 -- - -- .... 76 7.90 8.05 7.88 8.16 8.32 8.26 8.23 8.20 8.24 8.50 8.20 8.49 8.48 8.46 8.57 8.10 8.27 8.49 8.25 117.81 107.95 118.46 119.90 108.36 120.23 119.97 120.23 120.78 109.45 119.90 108.97 117.44 120.42 108.60 122.40 117.35 119.88 107.80 -- . . . . . . . . . . -- -- -- -- 77 78 79 80 81 82 83 84 85 86 87 88 89 90 91 92 93 94 95 96 96 97 98 99 100 101 102 . . 76 . .... 74 -- Appendix -- . . . . . . . ---- 60.90 43.79 54.03 54.71 43.52 54.91 54.24 54.07 54.16 43.08 54.11 43.09 53.29 53.55 43.97 55.41 58.47 56.57 44.73 -- -30.38 30.43 -27.87 -28.27 28.61 -30.84 -26.80 38.60 -40.09 35.55 26.05 -- -- . . 117.81 107.95 118.46 119.90 108.36 120.23 119.97 120.23 120.78 109.45 119.90 108.97 117.44 120.42 108.60 122.40 117.35 119.88 107.80 - ---- . . . . . . . -- -- -- 103 114.15 8.01 58.31 61.06 104 -- -- -- -- -- 105 106 107 108 109 110 111 112 119.24 121.76 116.47 115.40 117.54 118.60 122.23 120.24 8.73 7.91 7.88 8.13 7.91 8.06 8.00 7.89 54.84 52.42 53.98 54.76 54.17 53.93 50.03 50.44 37.94 16.31 40.09 25.81 30.35 27.13 17.39 39.43 119.24 121.76 116.47 115.40 117.54 118.60 122.23 120.24 113 114 --- --- --- --- --- 115 126.07 7.97 54.90 29.36 126.07 Table A4:Assignmt ofTCR 114.15 bd toLMPG-nia& at 310K 209 Appendix 210 Appendix Publications 1. Duchardt, E.; Richter, C; Reif, B.; Glaser, S. J.; Engels, J. W.; Griesinger, G.; Schwalbe, H (1999)"Measurement of nJ(H,)-Coupling Constants by Selective HC(C)H-TOCSY in Uniformly 13CLabeled RNA",J. Biwd NMR 21,117-126. 2. Waser, M.; Rueping, M.; Seebach, D.; Duchardt, E.; Schwalbe, H (2001) "On the solution structure of PHB - Preparation and NIMvRAnalysis of Isotopically Labeled Oligo ((R)-3hydroxybutanoic acids) (OHBs)", Hdv Cim Acta 84, 1821-1845. 3. Gee, P. J.; Hamprecht, F. A.; Schuler, L. D.; Van Gunsteren, W. F.; Duchardt, E.; Schwalbe, HI.;Albert, M.; Seebach, D. (2002) "A molecular dynamics simulation study of the conformational preferences of oligo-(3-hydroxyalcanoic acids) in chloroform solution.", Hdv Cbim Acta 85, 618-632. 4. Albert, M.; Seebach, D.; Duchardt, E.; Schwalbe, H (2002) "Synthesis and NMR Analysis in Solution of Oligo(3-hydroxyalkanoates) with the Side Chains of Alanine, Valine, and Leucine - Coming Full Circle from PHB to -Peptides to PHB.", Hdv Cim ACa 85, 633658. 5. Klein-Seetharaman, J.; Oikawa, M.; Grimshaw, S. B.; Winrmer, J.; Duchardt, E.; Ueda, T.; Imoto, T.; Smith, L. C; Dobson, C M; Schwalbe, H (2002) "Long-range interactions within a non-native protein", Sdexe 265, 1917-1921. 6. Duchardt, E.; Richter, C.; Ohlenschliger, (2004) "Determination of angle .; G6rlach, M; Wthnert, J.; Schwalbe, H in RNA from cross-correlated relaxation of CH-dipolar coupling and N-chemical shift anisotropy" J.Am (Cem Sc 126, 1962-1970. 7. Duchardt, E.; Schwalbe, FL (2004) "Residue specific dynamic investigation cUUCGgtetraloop motif by NMR 3C relaxation"J. Am 211 man Sc , submitted. of the