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

MOLECULAR

PHARMACOLOGY

May 2003Volume 63Number 5 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, Roth961

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-Poirot973

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 Chen983

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. Miller993

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 Cheng1002

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 Schumacher1012

Identification of Essential Residues Involved in the Allosteric Modulation of the Human A3 Adenosine Receptor

Zhan-Guo Gao, Soo-Kyung Kim, Ariel S. Gross, Aishe Chen, Joshua B. Blaustein, and
Kenneth A. Jacobson1021

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 Tigyi1032

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 Ryu1043

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 Biasi1059

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 Elgoyhen1067

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. Markillie1075

[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. Lesage1082

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 Borst1094

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. Perez1104

Potent Inhibition of Human Telomerase by Nitrostyrene Derivatives

Joo Hee Kim, Jun Hyun Kim, Gun Eui Lee, Jong Eun Lee, and In Kwon Chung1117

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 Wada1125

Characterization of Pulmonary CYP4B2, Specific Catalyst of Methyl Oxidation of 3-Methylindole

Brian A. Carr, Swayampakula Ramakanth, Ghazi A. Dannan, and Garold S. Yost1137

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 Muller1148

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. Jensen1159

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. Grady1169

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 Harden1190

Correction to "Cytochrome P450 3A conjugation to ubiquitin in a process distinct from classical

ubiquitination pathway"1198