MOLECULAR
PHARMACOLOGY
______________________________________
September 2004
Volume 66
Number 3
http://molpharm.aspetjournals.org
ISSN 0026-895X
PERSPECTIVE
Arrestin-Independent Internalization of G Protein-Coupled Receptors M
Chris J. van Koppen and Karl H. Jakobs
365
ARTICLES
COX-2 Regulates the Insulin-Like Growth Factor I-Induced Potentiation of Zn 3+-Toxicity in Primary
Cortical Culture
Joo-Young Im, Doyeun Kim, Kang-Woo Lee, Jung-Bin Kim, Ja-Kyeong Lee, Dong Sik Kim,
Young Ik Lee, Kwon-Soo Ha, Cheol O Joe, and Pyung-Lim Han
368
Agonist-Induced Internalization of Leukotriene B 4 Receptor 1 Requires G-Protein-Coupled Receptor
Kinase 2 but Not Arrestins
Zhangguo Chen, Remi Gaudreau, Christian Le Gouill, Marek Rola-Pleszczynski. and
Jana Stankovd
377
Rapid Regulation of P-Glycoprotein at the Blood-Brain Barrier by Endothelin-1
Anika M. S. Hartz, Bjbrn Bauer, Gert Fricker, and David S. Miller
387
Regulation of the Stability of P-Glycoprotein by Ubiquitination
Zhigang Zhang, Jin-Ying Wu, William N. Halt, and Jin-Ming Yang
395
Antisense Evidence for Nuclear Factor-tcB-Dependent Embryopathies Initiated by Phenytoin-Enhanced
Oxidative Stress
Julia C. Kennedy, Sylvie Memet, and Peter G. Wells
404
Pregnane X Receptor Up-Regxilation of P-Glycoprotein Expression and Transport Function at the
Blood-Brain Barrier
Bjb'rn Bauer, Anika M. S, Hartz, Gert Fricker, and David S. Miller
413
The al Nicotinic Acetylcholine Receptor Subunit Exists in Two Isoforms that Contribute to Functional
Ligand-Gated Ion Channels
Emily G. Severance, Hongling Zhang, Yolmari Cruz, Sergei Pakhlevaniants, Stephen H. Hadley,
Jahanshah Amin, Lynn Wecker, Crystal Reed, and Javier Cuevas
420
Mutation E522K in Human DNA Topoisomerase II/3 Confers Resistance to Methyl JV-(4'-(9acridinylamino)-phenyl)carbamate hydrochloride and Methyl A^-(4r-(9-acridinylamino)-3-methoxyphenyl) methane sulfonamide but Hypersensitivity to Etoposide
Chrysoula Leontiou, Jeremy H. Lakey, and Caroline A. Austin
430
Enhancement of Fibronectin Fibrillogenesis and Bone Formation by Basic Fibroblast Growth Factor
via Protein Kinase C-Dependent Pathway in Rat Osteoblasts
Chih-Hsin Tang, Rong-Sen Yang, Tsang-Hai Huang, Shing-Hwa Liu, and Wen-Mei Fu
440
Prediction of in Vivo Biliary Clearance from the in Vitro Transcellular Transport of Organic Anions
across a Double-Transfected Madin-Darby Canine Kidney II Monolayer Expressing Both Rat
Organic Anion Transporting Polypeptide 4 and Multidrug Resistance Associated Protein 2
Makoto Sasaki, Hiroshi Suzuki, Jun Aoki, Kousei Ito, Peter J. Meier, and Yuichi Sugiyama
450
P-Glycoprotein Mediates Resistance to Histidine Kinase Inhibitors
Sonia Arora, Jin-Ming Yang, Ryutaro Utsumi, Tadashi Okamoto, Takashi Kitayama, and
William N. Rait
460
Activation and Inhibition of Neuronal G Protein-Gated Inwardly Rectifying K + Channels by P2Y
Nucleotide Receptors
Alexander K. Filippov, Jose M. Fernandez-Fernandez, Stephen J. Marsh, Joseph Simon,
Eric A. Barnard, and David A. Brown
468
DNA Damage Induced by Temozolomide Signals to both ATM and ATR: Role of the Mis match Repair
System
Simona Caporali, Sabrina Falcinelli, Giuseppe Starace, Maria Teresa Russo, Enzo Bonmassar,
Josef Jiricny, and Stefania DAtri
478
3-Morpholinylsydnonimine Inhibits Glutamatergic Transmission in Rat Rostral Ventrolateral Medulla
via Peroxynitrite Formation and Adenosine Release
Chiung-Chun Huang, Samuel H. H. Chan, and Kuei-Sen Hsu
492
2,3,7,8-Tetrachlorodibenzo-p-dioxin Blocks Androgen-Dependent Cell Proliferation of LNCaP Cells
through Modulation of pRB Phosphorylation
Sonya Barnes-Ellerbe, Karen E. Knudsen, and Alvaro Puga
502
2,3,7,8-Tetrachlorodibenzo-p-dioxin Activation of the Aryl Hydrocarbon Receptor/Aryl Hydrocarbon
Receptor Nuclear Translocator Pathway Causes Developmental Toxicity through a CYP1A Independent Mechanism in Zebrafish
Sara A. Carney, Richard E. Peterson, and Warren Heideman
512
Dissociation of [ 3H]L-Glutamate Uptake from L-Glutamate-Induced [3H]D-Aspartate release by 3Hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-c?]isoxazole-4-carboxyric Acid and 3-Hydroxy-4,5,6,6atetrahydro-3ai/-pyrrolo[3,4-d]isoxazole-6-carboxylic Acid, Two Conformationally Constrained
Aspartate and Glutamate Analogs
Marcella Funicello, Paola Conti, Marco De Amid, Carlo De Micheli, Tiziana Mennini, and
Marco Gobbi
522
The Two-Pore-Domain K + Channels TREK-1 and TASK-3 Are Differentially Modulated by Copper and
Zinc
Marco Gruss, Alistair Mathie, William R. Lieb, and Nicholas P. Franks
530
Cholinergic Drugs for Alzheimer's Disease Enhance in Vitro Dopamine Release
Lifen Zhang, Fu-Ming Zhou, and John A. Dani
538
Key Differences in Molecular Complexes of the Cholecystokinin Receptor with Structurally Related
Peptide Agonist, Partial Agonist, and Antagonist
Sonnet J. H. Arlander, Maoqing Dong, Xi-Qin Ding, Delia I. Pinon, and Laurence J. Miller
545
Induction of Radiosensitization by Indolocarbazole Derivatives: The Role of DNA Topoisomerase I
Allan Y. Chen, Skyh-Jen Shih, Michael Hsiao, Mace L. Rothenberg, and Michelle Prudhomme
553
YC-1-Induced Cyclooxygenase-2 Expression Is Mediated by cGMP-Dependent Activations of Ras,
Phosphoinositide-3- OH-kinase, Akt, and Nuclear Factor-KB in Human Pulmonary Epithelial Cells
Ming-Shyan Chang, Wen-Sen Lee, Bing-Chang Chen, Joen-Rong Sheu, and Chien-Huang Lin
561
Effects of Antisense Oligonucleotide-Mediated Depletion of Tumor Necrosis Factor (TNF) Receptor 1Associated Death Domain Protein on TNF-Induced Gene Expression
Andrew M. Siwkowski, Lisa A. Madge, Seongjoon Koo, Erin L. McMillan, Brett P. Monia,
Jordan S. Pober, and Brenda F. Baker
572
Low Concentrations of Vinflunine Induce Apoptosis in Human SK-N-SH Neuroblastoma Cells through a
Postmitotic G± Arrest and a Mitochondrial Pathway
Bertrand Pourroy, Manon Carre, Stephane Honore, Veronique Bourgarel-Eey, Anna Kruczynski,
Claudette Briand, and Diane Braguer
580
Nordihydroguaiaretic Acid Does Not Disaggregate /3-Amyloid(l-40) Protofibrils but Does Inhibit
Growth Arising from Direct Protofibril Association
Melissa A. Moss, Nicholas H. Varvel, Michael R. Nichols, Dana Kim Reed, and
Terrone L. Rosenberry
592
Identification of the P2Y12 Receptor in Nucleotide Inhibition of Exocytosis from Bovine Chromaffm
Cells
Steven J. Ennion, Andrew D. Powell, and Elizabeth P. Seward
601
Berberine Inhibits HIF-la Expression via Enhanced Proteolysis
Shankung Lin, Shiow-Chwen Tsai, Chun-Chung Lee, Bao-Wei Wang, Jer-Young Liou, and
Kou-Gi Shyu
612
Small Interfering RNA-Mediated Suppression of dUTPase Sensitizes Cancer Cell Lines to Thymidylate
Synthase Inhibition
Sara E. Koehler and Robert D. Ladner
620
DNA Topoisomerase I As One of the Cellular Targets of Certain Tyrphostin Derivatives
Sarit Bendetz-Nezer, Aviv Gazit, and Esther Priel
627
A Vascular Endothelial Growth Factor Receptor-2 Kinase Inhibitor Potentiates the Activity of the
Conventional Chemotherapeutic Agents Paclitaxel and Doxorubicin in Tumor Xenograft Models
Stuart Emanuel, Robert H. Gruninger, Angel Fuentes-Pesquera, Peter J. Connolly,
Jennifer A, Seamon, Susan Hazel, Rose Tominovich, Beth Hollister, Cheryl Napier,
Michael R. D'Andrea, Michael Reuman, Gilles Bignan, Robert Tuman, Dana Johnson,
David Moffatt, Mark Batchelor, Anne Foley, James O'Connell, Rodger Allen, Martin Perry,
Linda Jolliffe, and Steven A. Middleton
635
Lidocaine: A Foot in the Door of the Inner Vestibule Prevents Ultra-Slow Inactivation of a VoltageGated Sodium Channel
Walter Sandtner, Julia Szendroedi, Touran Zarrabi, Eva Zebedin, Karlheinz Hilber, Ian Glaaser,
Harry A. Fozzard, Samuel C. Dudley, and Hannes Todt
648
Regulation of Nicotinic Acetylcholine Receptor Channel Function by Acetylcholinesterase In hibitors in
Rat Hippocampal CA1 Interneurons
Dmitriy Fayuk and Jerrel L. Yakel
658
y-Mangostin Inhibits Inhibitor-KB Kinase Activity and Decreases Lipopolysaccharide-Induced
Cyclooxygenase-2 Gene Expression in C6 Rat Glioma Cells
Keigo Nakatani, Tohru Yamakuni, Nobuhiko Kondo, Tsutomu Arakawa, Kenji Oosawa,
Susumu Shimura, Hiroyasu Inoue, and Yasushi Okizumi
667
Enantioselective Effects of Hydroxy Metabolites of Bupropion on Behavior and on Function of
Monoamine Transporters and Nicotinic Receptors
M. Imad Damaj, F. Ivy Carroll, J. Brek Eaton, Hernan A. Navarro, Bruce E. Blough, Sadiq Mirza,
Ronald J. Lukas, and Billy R. Martin
675
Flavonoids Inhibit Tumor Necrosis Factor-a-Induced Up-Regulation of Intercellular Adhesion Molecule-1
(ICAM-1) in Respiratory Epithelial Cells through Activator Protein-1 and Nuclear Factor-KB:
Structure-Activity Relationships
Ching-Chow Chen, Man-Ping Chow, Wei-Chien Huang, Yi-Chu Lin, and Ya-Jen Chang
683
Role of Liver-Enriched Transcription Factors in the Down-Regulation of Organic Anion Transporting
Polypeptide 4 (Oatp4; Oatplb2; Slc21alO) by Lipopolysaccharide
Ning Li and Curtis D. Klaassen
694
Diethylstilbestrol Is a Potent Inhibitor of Store-Operated Channels and Capacitative Ca 2+ Influx
Sergey I. Zakharov, Tarik Smani, Yuliya Dobrydneva, Francisco Monje, Craig Fichandler,
Peter F. Blackmore, and Victoria M. Bolotina
702
The Myosin ATPase Inhibitor 2,3-Butanedione monoxime Dictates Transcriptional Activation of Ion
Channels and Ca 2+ -Handling Proteins
Jiirgen Borlak and Carotin Zwadlo
708
The Role of Membrane and Vesicular Monoamine Transporters in the Neurotoxic and Hypothermic
Effects of l-Methyl-4- (2'-aminophenyl)-l,2,3,6-tetrahydropyridine (2'-NH2-MPTP)
Adam L. Numis, Erica L. linger, Douglas L. Sheridan, Angela C. Chisnell, and Anne M. Andrews
718
Acetaminophen: A Central Analgesic Drug That Involves a Spinal Tropisetron-Sensitive, Non-5-HT 3 ReceptorMediated Effect F. Libert, J. Bonnefont, E. Bourinet, E, Doucet, A. Alloui, M. Hamon, J. Nargeot, and A.
Eschalier
728
Evidence for a Novel K + Channel Modulated by a 1A-Adrenoceptors in Cardiac Myocytes
Stephanie C. M, Choisy, Jules C. Hancox, Lesley A. Arberry, A. Martyn Reynolds,
Michael J. Shattock, and Andrew F. James
735
Glutathione Depletion in CYP2El~Expressing Liver Cells Induces Toxicity Due to the Activation of p38
Mitogen-Activated Protein Kinase and Reduction of Nuclear Factor-KB DNA Binding Activity
Defeng Wu and Arthur Cederbaum
749
Functional Role of a C-Terminal G/37-Binding Domain of Ca v2.2 Channels
Bin Li, Huijun Zhong, Todd Scheuer, and William A. Catterall
761