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 A3 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
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