MOLECULAR

PHARMACOLOGY

August 2003Volume 64Number 2 0026-895X

ANNOUNCEMENT195

PERSPECTIVES

Center Stage for the Serotonin Transporter: A Gain of Function Polymorphism in Persons with
Obsessive-Compulsive Disorder OH
Gonzalo E. Torres and Marc G. Caron196

Sleuthful Pharmacology <§>

John S. Lazo, Alexander P. Ducruet, and Radosevda P. Koldamova199

ARTICLES

Painful Inflammation-Induced Increase in ^-Opioid Receptor Binding and G-Protein Coupling in
Primary Afferent Neurons
C. Zollner, M. A. Shaqura, C. P. Bopaiah, S. Mousa, C. Stein, and M. Schafer202

Inhibition of Nuclear Factor kB by Phenolic Antioxidants: Interplay between Antioxidant Signaling and
Inflammatory Cytokine Expression
Qiang Ma, Krista Kinneer, Jianping Ye, and Bruce J. Chen211

Antifolate Resistance Associated with Loss of MRP1 Expression and Function in Chinese Hamster Ovary Cells with Markedly Impaired Export of Folate and Cholate

Michal Stark, Lilah Rothem, Gerrit Jansen, George L. Scheffer, I. David Goldman, and
Yehuda G. Assaraf220

Calcium-Dependent Prevention of Neuronal Apoptosis by Lithium Ion: Essential Role of
Phosphoinositide 3-Kinase and Phospholipase Cy
Hyo Jung Kang, Jai Sung Noh, Yun Soo Bae, and Byoung Joo Gwag228

Key Roles of Phe1112 and Ser1115 in the Pore-Forming IIIS5-S6 Linker of L-Type Ca2+ Channel aic Subunit (Cav1.2) in Binding of Dihydropyridines and Action of Ca2+ Channel Agonists Shinji Yamaguchi, Boris S. Zhorov, Katsuro Yoshioka, Taku Nagao, Hidenori Ichijo, and

Satomi Adachi-Akahane235

Prostacylin Receptor Activation Inhibits Proliferation of Aortic Smooth Muscle Cells by Regulating cAMP Response Element-Binding Protein- and Pocket Protein-Dependent Cyclin A Gene Expression

Devashish Kothapalli, Sheryl A. Stewart, Emer M. Smyth, Ijeoma Azonobi, Ellen Pure, and

Richard K. Assoian249

Anticancer Drug Resistance Induced by Disruption of the Saccharomyces cerevisiae NPR2 Gene: a
Novel Component Involved in Cisplatin- and Doxorubicin-Provoked Cell Kill
Paul W. Schenk, Mariel Brok, Antonius W. M. Boersma, Jourica A. Brandsma, Hans Den Dulk,
Herman Burger, Gerrit Stoter, Jaap Brouwer, and Kees Nooter259

The Mechanism of Action of Aniracetam at Synaptic a-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic
Acid (AMPA) Receptors: Indirect and Direct Effects on Desensitization
J. Josh Lawrence, Stephan Brenowitz, and Laurence O. Trussell269

Carboxylesterase-Mediated Sensitization of Human Tumor Cells to CPT-11 Cannot Override ABCG2-Mediated Drug Resistance

Monika Wierdl, Amelia Wall, Christopher L. Morton, Janardhan Sampath, Mary K. Banks,
John D. Schuetz, and Philip M. Potter279

P53-Dependent Cell-Killing by Selective Repression of Thymidine Kinase and Reduced Prodrug Activation

Dong Xu, Deitmar Falke, and R. L. Juliano289

Isoprostane-Mediated Secretion from Human Airway Epithelial Cells

Elizabeth A. Cowley298

c-Jun NH2-Terminal Kinase Inhibitor Anthra<l,9-cc/)pyrazol-6(2H)-one Reduces Inducible Nitric-Oxide
Synthase Expression by Destabilizing mRNA in Activated Macrophages
Aleksi Lahti, Ulla Jalonen, Hannu Kankaanranta, and Eeva Moilanen308

Identification of Constitutive Androstane Receptor and Glucocorticoid Receptor Binding Sites in the CYP2C19 Promoter

Yuping Chen, Stephen S. Ferguson, Masahiko Negishi, and Joyce A, Goldstein316

High-Affinity Partial Agonists of the Vanilloid Receptor

Yun Wang, Attila Toth, Richard Tran, Tamas Szabo, Jacqueline D. Welter, Peter M. Blumberg,

Jiyoun Lee, Sang-Uk Kang, Ju-Ok Lim, and Jeewoo Lee325

Preservation of Caspase-3 Subunits from Degradation Contributes to Apoptosis Evoked by Lactacystin:
Any Single Lysine or Lysine Pair of the Small Subunit Is Sufficient for Ubiquitination
Lei Chen, Lucinda Smith, Zhi Wang, and Jeffrey B. Smith334

Oltipraz Is a Bifunctional Inducer Activating Both Phase I and Phase II Drug-Metabolizing Enzymes
via the Xenobiotic Responsive Element
Weimin Miao, Lianggao Hu, Mustapha Kandouz, and Gerald Batist346

Down-Regulation of STAT5b Transcriptional Activity by Ligand-Activated Peroxisome Proliferator-
Activated Receptor (PPAR) a and PPAR-y
Jonathan M. Shipley and David J. Waxrnan355

Cholesterol Antagonizes Ethanol Potentiation of Human Brain BKca Channels Reconstituted into
Phospholipid Bilayers
John J. Crowley, Steven N. Treistman, and Alejandro M. Dopico365

Isoflurane and Propofol Inhibit Voltage-Gated Sodium Channels in Isolated Rat Neurohypophysial
Nerve Terminals
Wei OuYang, Gang Wang, and Hugh C. Hemmings, Jr.373

Molecular Modes of Action of Artesunate in Tumor Cell Lines

Thomas Efferth, Axel Sauerbrey, Armin Olbrich, Erich Gebhart, Pia Rauch, H. Oliver Weber,

Jan G. Hengstler, Marc-Eric Halatsch, Manfred Volm, Kenneth D. Tew, Douglas D. Ross, and

Jens Oliver Funk382

Desensitization of a-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors Facilitates Use-Dependent Inhibition by Pentobarbital

Michael F. Jackson, Daisy T. Joo, Azza A. Al-Mahrouki, Beverley A. Orser, and
John F. MacDonald395

Aspirin Protects Caco-2 Cells from Apoptosis after Serum Deprivation through the Activation of a Phosphatidylinositol 3-Kinase/AKT/p21c'WWAF1 Pathway

Paolo Ricchi, Antonella di Palma, Tiziana Di Matola, Anna Apicella, Rosaria Fortunato,
Raffaele Zarrilli, and Angela Maria Acquaviva407

Thalidomide Down-Regulates Transcript Levels of GC-Rich Promoter Genes in Multiple Myeloma

Liat Drucker, Orit Uziel, Tali Tohami, Hava Shapiro, Judith Radnay, Shai Yarkoni, Meir Lahav,

and Michael Lishner415

Differential Involvement of Intracellular Domains of the Rat NTS1 Neurotensin Receptor in Coupling to G Proteins: A Molecular Basis for Agonist-Directed Trafficking of Receptor Stimulus

Delphine Skrzydelski, Anne-Marie Lhiaubet, Antony Lebeau, Patricia Forgez, Misa Yamada,

Emmanuel Hermans, William Rostene, and Didier Pelaprat421

Dissociation of High-Affinity Cocaine Analog Binding and Dopamine Uptake Inhibition at the Dopamine Transporter

Wenfei Wang, Mark S. Sonders, Okechukwu T. Ukairo, Helen Scott, Megan K, Kloetzel, and

Christopher K. Surratt,430

A Human Serotonin Transporter Mutation Causes Constitutive Activation of Transport Activity

Fusun Kilic, Dennis L. Murphy, and Gary Rudnick440

Requirement of G/3y and c-Src in D2 Dopamine Receptor-Mediated Nuclear Factor-KB Activation

Ming Yang, Hongmei Zhang, Tatyana Voyno-Yasenetskaya, and Richard D. Ye447

Msh2 Deficiency Abrogates But Does Not Abolish Thiopurine Hematopoietic Toxicity in Msh2~'~ Mice
Natalia F. Krynetskaia, Timothy L. Brenner, F.ugene Y. Krynetski, Weinan Du, John C. Panetta,
Ching-Hon Pui, and William E. Evans456

The Copper Export Pump ATP7B Modulates the Cellular Pharmacology of Carboplatin in Ovarian Carcinoma Cells

Kuniyuki Katano, Roohangiz Safaei, Goli Samimi, Alison Holzer, Myriam Rochdi, and
Stephen B. Howell466

The Environmental Pollutant l,l-Dichloro-2,2-bis (p-chlorophenyl)ethylene Induces Rat Hepatic Cytochrome P450 2B and 3A Expression through the Constitutive Androstane Receptor and Pregnane X Receptor

Michael E, Wyde, Erika Bartolucci, Akiko Ueda, He Zhang, Binfang Yan, Masahiko Negishi, and
Li You474

Polymorphisms in Human Soluble Epoxide Hydrolase

Beata D. Przybyla-Zawislak, Punit K. Srivastava, Johana Vdzquez-Matias,

Harvey W. Mohrenweiser, Joseph E. Maxwell, Bruce D. Hammock, J. Alyce Bradbury,

Ahmed E. Enayetallah, Darryl C. Zeldin, and David F. Grant482

Molecular Determinants of Ca2+ Potentiation of Diltiazem Block and Ca2+-Dependent Inactivation in
the Pore Region of Cav1.2
Nejmi Dilmac, Nathan Hilliard, and Gregory H. Hockerman491

Prevalence of Necrosis in C2-Ceramide-Induced Cytotoxicity in NB16 Neuroblastoma Cells

Belen Ramos, Jill M. Lahti, Enrique Claro, and Suzanne Jackowski502

Tiotidine, a Histamine H2 Receptor Inverse Agonist That Binds with High Affinity to an Inactive G-Protein-Coupled Form of the Receptor. Experimental Support for the Cubic Ternary Complex Model

Federico Monczor, Natalia Fernandez, Bibiana Lemos Legnazzi, Maria Eugenia Riveiro,
Alberto Baldi, Carina Shayo, and Carlos Davio512

cGMP/Protein Kinase G-Dependent Potentiation of Glutamatergic Transmission Induced by Nitric
Oxide in Immature Rat Rostral Ventrolateral Medulla Neurons in Vitro
Chiung-Ckun Huang, Samuel H. H. Chan, and Kuei-Sen Hsu521