An Array of Details on G-Protein Coupled Receptor Signaling: Differential Effects of A

MOLECULAR PHARMACOLOGY May 2003 Volume 63 Number 5 http://molpharm.aspetjournals.org ISSN 0026-895X

PERSPECTIVE An Array of Details on G-Protein Coupled Receptor Signaling: Differential Effects of a^-Adrenergic Receptor Subtypes on Gene Expression and Cytokine Receptor Signaling 13 Neil M. Nathanson 959 ARTICLES

The Interaction of a Constitutively Active Arrestin with the Arrestin-Insensitive 5-HT2A Receptor Induces Agonist-Independent Internalization John A. Gray, Anushree Bhatnagar, Vsevolod V. Gureuich, and Bryan L, Roth 961

Identification of Tyrosine 189 and Asparagine 358 of the Cholecystokinin 2 Receptor in Direct Interaction with the Crucial C-Terminal Amide of Cholecystokinin by Molecular Modeling, Site-Directed Mutagenesis, and Structure/Affinity Studies Celine Gales, Marc Poirot, Julien Taillefer, Bernard Maigret, Jean Martinez, Luis Moroder, Chantal Escrieut, Lucien Pradayrol, Daniel Fourmy, and Sandrine Silvente-Poirot 973

Activation and Binding of Peroxisome Proliferator-Activated Receptor y by Synthetic Cannabinoid Ajulemic Acid Jilin Liu, Hui Li, Sumner H. Burstein, Robert B. Zurier, and J. Don Chen 983

Spatial Approximation between a Photolabile Residue in Position 13 of Secretin and the Amino Terminus of the Secretin Receptor Mengwei Zang, Maoqing Dong, Delia I. Pinon, Xi-Qin Ding, Elizabeth M. Hadac, Zhijun Li, Terry P. Lybrand, and Laurence J. Miller 993

Crucial Role of Extracellular Signal-Regulated Kinase Pathway in Reactive Oxygen Species-Mediated Endothelin-1 Gene Expression Induced by Endothelin-1 in Rat Cardiac Fibroblasts Cheng-Ming Cheng, Hong-Jye Hong, Ju-Chi Liu, Neng-Lang Shih, Shu-Hui Juan, Shih-Hurng Loh, Paul Chan, Jin-Jer Chen, and Tzu-Hurng Cheng 1002

Glucocorticoid Receptor Antagonism by Cyproterone Acetate and RU486 Christian Honer, Kiyean Nam, Cynthia Fink, Paul Marshall, Gary Ksander, Ricardo E. Chatelain, Wendy Cornell, Ronald Steele, Robert Schweitzer, and Christoph Schumacher 1012 Identification of Essential Residues Involved in the Allosteric Modulation of the Human A 3 Adenosine Receptor Zhan-Guo Gao, Soo-Kyung Kim, Ariel S. Gross, Aishe Chen, Joshua B. Blaustein, and Kenneth A. Jacobson

1021 Fatty Alcohol Phosphates Are Subtype-Selective Agonists and Antagonists of Lysophosphatidic Acid Receptors Tamas Virag, Don B. Elrod, Karoly Liliom, Vineet M. Sardar, Abby L. Parrill, Kazuaki Yokoyama, Gangadhar Durgam, Wenlin Deng, Duane D. Miller, and Gabor Tigyi 1032 Identification of a Compound That Directly Stimulates Phospholipase C Activity Yoe-Sik Bae, Taehoon G. Lee, Jun Chut Park, Jung Ho Hur, Youndong Kim, Kyun Heo, Jong-Young Kwak, Pann-Ghill Suh, and Sung Ho Ryu 1043 Voltage-Dependent Profile of Human Ether-a-go-go-Related Gene Channel Block Is Influenced by a Single Residue in the S6 Transmembrane Domain Jose A. Sdnchez-Chapula, Tania Ferrer, Ricardo A. Navarro- Polanco, and Michael C. Sanguinetti 1051 The Nicotinic Acetylcholine Receptor Subunit a5 Mediates Short-Term Effects of Nicotine in Vivo Ramiro Salas, Avi Orr-Urtreger, Ron S. Broide, Arthur Beaudet, Richard Paylor, and Mariella De Biasi 1059 Direct Interaction of Serotonin Type 3 Receptor Ligands with Recombinant and Native «9alO-Containing Nicotinic Cholinergic Receptors Carla V. Rothlin, Maria I. Lioudyno, Ana F, Silbering, Paola V. Plazas, Maria E. Gomez Casati, Eleonora Katz, Paul S. Guth, and A. Belen Elgoyhen 1067

Regulation of Activator Protein-1 by 8-iso-Prostaglandin E2 in a Thromboxane A2 Receptor-Dependent and -Independent Manner Thomas J. Weber and Lye M. Markillie 1075 [3H]R214127: A Novel High-Affinity Radioligand for the mGlul Receptor Reveals a Common Binding Site Shared by Multiple Allosteric Antagonists Hilde Lavreysen, Cor Janssen, Francois Bischoff, Xavier Langlois, Josee E, Leysen, and Anne S, J. Lesage 1082 Characterization of the Transport of Nucleoside Analog Drugs by the Human Multidrug Resistance Proteins MRP4 and MRP5 Glen Reid, Peter Wielinga, Noam Zelcer, Marcel de Haas, Liesbeth van Deemter, Jan Wijnholds, Jan Balzarini, and Piet Borst 1094 M Genetic Profiling of o^-Adrenergic Receptor Subtypes by Oligonucleotide Microarrays: Coupling to Interleukin-6 Secretion but Differences in STAT3 Phosphorylation and gp-130 Pedro J. Gonzalez-Cabrera, Robert J. Gaivin, June Yun> Sean A. Ross, Robert S. Papay, Dan F. McCune, Boyd R. Rorabaugh, and Dianne M. Perez 1104 Potent Inhibition of Human Telomerase by Nitrostyrene Derivatives Joo Hee Kim, Jun Hyun Kim, Gun Eui Lee, Jong Eun Lee, and In Kwon Chung 1117

Destabilization of Nav1.7 Sodium Channel a-Subunit mRNA by Constitutive Phosphorylation of Extracellular Signal-Regulated Kinase: Negative Regulation of Steady-State Level of Cell Surface Functional Sodium Channels in Adrenal Chromafiin Cells Toshihiko Yanagita, Hideyuki Kobayashi, Yasuhito Uezono, Hiroki Yokoo, Takashi Sugano, Tomokazu Saitoh, Shin-Ichi Minami, Seiji Shiraishi, and Akihiko Wada 1125 Characterization of Pulmonary CYP4B2, Specific Catalyst of Methyl Oxidation of 3-Methylindole Brian A. Carr, Swayampakula Ramakanth, Ghazi A. Dannan, and Garold S. Yost 1137 Role of S-Nitrosation of Cysteine Residues in Long-Lasting Inhibitory Effect of Nitric Oxide on Arterial Tone Jacicarlos L. Alencar, Irina Lobysheva, Michel Geffard, Mamadou Sarr, Christa Schott, Valerie B. Schini-Kerth, Franqoise Nepveu, Jean-Claude Stoclet, and Bernard Muller 1148 Probing the Role of Linker Substituents in Bisdioxopiperazine Analogs for Activity against Wild-Type and Mutant Human Topoisomerase Ha Axelle Renodon-Comiere, Tina K. S0rensen, Peter B. Jensen, John L. Nitiss, Birgitte S0kilde, Maxwell Sehested, and Lars H. Jensen

1159 Differential Declines in Striatal Nicotinic Receptor Subtype Function after Nigrostriatal Damage in Mice Maryka Quik, Jocelyn D. Sum, Paul Whiteaker, Sarah E. McCallum, Michael J. Marks, John Musachio, J. Michael Mclntosh, Allan C. Collins, and Sharon R. Grady

1169 Transcriptional Regulation of Human CYP3A4 Basal Expression by CCAAT Enhancer-Binding Protein a and Hepatocyte Nuclear Factor-3y C. Rodriguez-Antona, R. Bort, R. Jover, N. Tindberg, M. Ingelman-Sundberg, M. J. Gomez-Lechon, and J. V. Castell . 1180 Release of Cellular UDP-Glucose as a Potential Extracellular Signaling Molecule Eduardo R. Lazarowski, Deborah A. Shea, Richard C. Boucher, and T. Kendall Harden

1190 Correction to "Cytochrome P450 3A conjugation to ubiquitin in a process distinct from classical ubiquitination pathway" 1198