MOLECULAR
PHARMACOLOGY
March 2004
Volume 65
Number 3
http://molpharm.aspetjournals.org
ISSN 0026-895X
MINIREVIEW
The Molecular Pharmacology of Organic Anion Transporters: from DNA to FDA?
Satish A. Eraly, Kevin T. Bush, Rosemary V. Sampogna, Vibha Bhatnagar, and Sanjay K, Nigam
479
PERSPECTIVES
The Confluence of Population Genetics with Molecular Pharmacology at the Angiotensin II Receptor:
Dawn of a New Era or Just a New Wrinkle? M
Morton P. Printz
488
Receptor Domains Regulating /J. Opioid Receptor Uncoupling and Internalization: Relevance to Opioid
Tolerance <§>
Brian M. Cox and A. Tamara Crowder
492
ARTICLES
Identification of Novel Alternative Splice Variants of Human Constitutive Androstane Receptor and
Characterization of Their Expression in the Liver
Hideto Jinno, Toshiko Tanaka-Kagawa, Nobumitsu Hanioka, Seiich Ishida, Mayumi Saeki,
Akiko Soyama, Masaya Itoda, Tetsuji Nishimura, Yoshiro Saito, Shogo Ozawa, Masanori Ando,
and Jun-ichi Sawada
496
Functional Role of Lipid Raft Microdomains in Cyclic Nucleotide-Gated Channel Activation
James D. Brady, Thomas C. Rich, Xuan Le, Kimberlee Stafford, Cedar J. Fowler, Leatha Lynch,
Jeffrey W. Karpen, R. Lane Brown, and Jeffrey R. Martens
503
Functional and Genetic Diversity in the Concentrative Nucleoside Transporter, CNT1, in Human
Populations
Jennifer H. Gray, Lara M. Mangravite, Ryan P. Owen, Thomas J. Urban, Wendy Chan,
Elaine J. Carlson, Conrad C. Huang, Michiko Kawamoto, Susan J. Johns, Douglas Stryke,
Thomas E. Ferrin, and Kathleen M. Giacomini
512
Valproic Acid Inhibits Angiogenesis in Vitro and in Vivo
Martin Michaelis, U. Ruth Michaelis, Ingrid Fleming, Tatyana Suhan, Jaroslav Cinatl,
Roman A. Blaheta, Katrin Hoffmann, Rouslan Kotchetkov, Rudi Busse, Heinz Nau, and
Jindrich Cinatl Jr.
520
Distinct Domains of the ^t-Opioid Receptor Control Uncoupling and Internalization
Jeremy Celver, Mei Xu, Wenzhen Jin, Janet Lowe, and Charles Chavkin
528
8R-Lisuride Is a Potent Stereospecific Histamine H 1-Receptor Partial Agonist
R. A. Bakker, D. M. Weiner, T. ter Laak, T Beuming, O. P. Zuiderveld, M. Edelbroek, U. Hacksell,
H. Timmerman, M. R. Brann, and R. Leurs
538
Retinoid X Receptor a Regulates Glutathione Homeostasis and Xenobiotic Detoxification Processes in
Mouse Liver
Yong Wu, Xiaoxue Zhang, Fawzia Bardag-Gorce, Rose C. V. Robel, Jonathan Aguilo, Lixin Chen,
Ying Zeng, Kelly Hwang, Samuel W. French, Shelly C. Lu, and Yu-Jui Y. Wan
550
Molecular Requirements of the Human Nucleoside Transporters hCNTl, hCNT2, and hENTl
C. Chang, P. W. Swaan, L. Y. Ngo, P. Y. hum, S. D. Patil, and J. D. Unadkat
558
Evidence of a Functional Role for ^21WAF1IC1P1 Down-Regulation in Synergistic Antileukemic
Interactions between the Histone Deacetylase Inhibitor Sodium Butyrate and Flavopiridol
Roberto R. Rosato, Jorge A. Almenara, Chunrong Yu, and Steven Grant
571
Structural Determinants Required for the Bioactivities of Prokineticins and Identification of
Prokineticin Receptor Antagonists
Clayton M. Bullock, Jia-Da Li, and Qun-Yong Zhou
582
Differential Role of Janus Family Kinases (JAKs) in Interferon-7-Induced Lung Epithelial ICAM-1
Expression: Involving Protein Interactions between JAKs, Phospholipase Cy, c -Src, and STAT1
Ya-Jen Chang, Michael J. Holtzman, and Ching-Chow Chen
589
Caffeic Acid Esters Activate TREK-1 Potassium Channels and Inhibit Depolarization-Dependent
Secretion
Sanjay Danthi, Judith A. Enyeart, and John J. Enyeart
599
Up-Regulation of Brain Nicotinic Acetylcholine Receptors in the Rat during Long -Term SelfAdministration of Nicotine: Disproportionate Increase of the a6 Subunit
Steven L. Parker, Yitong Fu, Kathleen McAllen, Jianhong Luo, J. Michael Mclntosh,
Jon M. Lindstrom, and Burt M. Sharp
611
Vasopressin Stimulates Insulin Release from Islet Cells through Vlb Receptors: a Combined
Pharmacological/Knockout Approach
Sayuri Oshikawa, Akito Tanoue, Taka-aki Koshimizu, Yoko Kitagawa, and Gozoh Tsujimoto
623
Blockage of Intermediate-Conductance C a 2+-Activated K + Channels Inhibit Human Pancreatic Cancer
Cell Growth in Vitro
Heike Jdger, Tobias Dreker, Anita Buck, Klaudia Giehl, Thomas Gress, and Stephan Grissmer
630
Dipyridamole Alters Cardiac Substrate Preference by Inducing Translocation of FAT/CD36, but Not
That of GLUT4
Joost J. F. P. Luiken, Susan L. M. Coort, Jodil Willems, Will A. Coumans, Arend Bo nen, and
Jan F. C. Glatz
639
Selective Knock-Down of P2X 7 ATP Receptor Function by Dominant-Negative Subunits
Ramin Raouf Yassar Chakfe, Dominique Blais, Audrey Speelman, Eric Boue-Grabot,
Duncan Henderson, and Philippe Seguela
646
Protein Adduct-Trapping by Hydrazinophthalazine Drugs: Mechanisms of Cytoprotection Against
Acrolein-Mediated Toxicity
Philip C. Burcham, Frank R. Fontaine, Lisa M. Kaminskas, Dennis R. Petersen, and
Simon M. Pyke
.
655
Endocannabinoids Modulate N-Type Calcium Channels and G-Protein-Coupled Inwardly Rectifying
Potassium Channels via CB1 Cannabinoid Receptors Heterologously Expressed in Mammalian
Neurons
Juan Guo and Stephen R. Ikeda
665
The Molecular Basis of the Action of Disulfiram as a Modulator of the Multidrug Resistance -Linked
ATP Binding Cassette Transporters MDR1 (ABCB1) and MRP1 (ABCC1)
Zuben E. Sauna, Xiang-Hong Peng, Krishnamachary Nandigama, Samrawit Tekle, and
Suresh V. Ambudkar
675
Combinatorial Interaction of Scorpion Toxins Lqh-2, Lqh-3, and LqhalT with Sodium Channel
Receptor Sites-3
Enrico Leipold, Songqing Lu, Dalia Gordon, Alfred Hansel, and Stefan H. Heinemann
685
Uptake Inhibitors but not Substrates Induce Protease Resistance in Extracellular Loop Two of the
Dopamine Transporter
Jon D. Gaffaney and Eoxanne A. Vaughan
692
Random Mutagenesis of the Human Adenosine A 2B Receptor Followed by Growth Selection in Yeast.
Identification of Constitutively Active and Gain of Function Mutations
Margot W. Beukers, Joris van Oppenraaij, Patrick P. W. van der Hoorn, Clara C. Blad,
Hans den Dulk, Jaap Brouwer, and Adriaan P. IJzerman
702
Expression of A 3 Adenosine Receptors in Human Lymphocytes: Up-Regulation in T Cell Activation
Stefania Gessi, Katia Varani, Stefania Merighi, Elena Cattabriga, Arianna Avitabile,
Riccardo Gavioli, Cinzia Fortini, Edward Leung, Stephen Mac Lennan, and Pier Andrea Borea
711
Dehydroepiandrosterone Sulfotransferase Is a Target for Transcriptional Induction by the Vitamin D
Receptor
Ibtissam Echchgadda, Chung S. Song, Arun K. Roy, and Bandana Chatterjee
720
Regulation of Mouse Renal CYP2J5 Expression by Sex Hormones
Jixiang Ma, Joan Graves, J. Alyce Bradbury, Yun Zhao, Deborah L, Swope, Lorraine King,
Wei Qu, James Clark, Page Myers, Vickie Walker, Jonathan Lindzey, Kenneth S. Korach, and
Darryl C. Zeldin
730
SB-505124 Is a Selective Inhibitor of Transforming Growth Factor-/3 Type I Receptors ALK4, ALK5,
and ALK7
Stacey DaCosta By field, Christopher Major, Nicholas J. Laping, and Anita B. Roberts
744
Ligand Function at Constitutively Active Receptor Mutants Is Affected by Two Distinct Yet Interacting
Mechanisms
Martin Beinborn, Yong Ren, Michael Bld'ker, Ci Chen, and Alan S. Kopin
753
DAXX, FLASH, and FAF-1 Modulate Mineralocorticoid and Glucocorticoid Receptor-Mediated
Transcription in Hippocampal Cells—Toward a Basis for the Opposite Actions Elicited by Two
Nuclear Receptors?
D. Obradovic, M. Tirard, Zs. Nemethy, O. Hirsch, H. Gronemeyer, and O. F. X. Almeida
761
H Loss-of-Function Polymorphic Variants of the Human Angiotensin II Type 1 Receptor
Jakob Lerche Hansen, Stig Hauns0, Mark R. Brann, S0ren P. Sheikh, and David M. Welner
Phorbol 12-Myristate 13-Acetate Protects Jurkat Cells from Methylglyoxal-Induced Apoptosis by
Preventing c-Jun N-Terminal Kinase-Mediated Leakage of Cytochrome c in an Extracellular
Signal-Regulated Kinase-Dependent Manner
Yoshikazu Takagi, Jun Du, Xiu-Yang Ma, Izumi Nakashima, and Fumihiko Nagase
770
778
An Apamin- and Scyllatoxin-Insensitive Isoform of the Human SK3 Channel
Oliver H. Wittekindt, Violeta Visan, Hiroaki Tomita, Faiqa Imtiaz, Jay J, Gargus,
Frank Lehmann-Horn, Stephan Grissmer, and Deborah J. Morris-Rosendahl
788
Effects of SEA0400 on Mutant NCX1.1 Na +-Ca2+ Exchangers with Altered Ionic Regulation
Ron Bouchard, Alexander Omelchenko, Hoa Dinh Le, Platon Choptiany, Toshio Matsuda,
Akemichi Baba, Kenzo Takahashi, Debora A. Nzcolt, Kenneth D. Philipson, Mark Hnatowich, and
Larry V. Hryshko
802
Correction to "Agonist binding and Gq-stimulating activities of the purified human P2Y a receptor"
811