New Insights Into G-Protein-Coupled Receptor Signaling from the Melanocortin Receptor System M

MOLECULAR PHARMACOLOGY July 2003 Volume 64 Number 1 http://molpharm.aspetjournals.org ISSN 0026-895X

PERSPECTIVE New Insights into G-Protein-Coupled Receptor Signaling from the Melanocortin Receptor System M Brinda K. Rana 1

ACCELERATED COMMUNICATION Identification of a Site in GluRl and GluR2 That Is Important for Modulation of Deactivation and Desensitization J. Duncan Leever, Suzanne Clark, Autumn M. Weeks, and Kathryn M. Partin 5 Spatial Regulation of Gai Protein Signaling in Clathrin-Coated Membrane Microdomains Containing GAIP Eric Elenko, Thierry Fischer, Ingrid Niesman, Tim Harding, Tammie McQuistan, Mark Von Zastrow, and Marilyn G. Farquhar 11 Allosteric Site on Muscarinic Acetylcholine Receptors: Identification of Two Amino Acids in the Muscarinic M2 Receptor That Account Entirely for the M2/M5 Subtype Selectivities of Some Structurally Diverse Allosteric Ligands in Af-Methylscopolamine- Occupied Receptors Uta Voigtldnder, Kirstin Johren, Marion Mohr, Alexandra Raasch, Christian Trdnkle, Stefan Buller, John Ellis, Hans-Dieter Holtje, and Klaus Mohr 21 Rescuing the Traffic-Deficient Mutants of Rat jx-Opioid Receptors with Hydrophobic Ligands Vipa Chaipatikul, Laurie J. Erickson-Herbrandson, Horace H. Loh, and Ping-Yee Law 32 Transgenic Mouse Models of Human CYP3A4 Gene Regulation Graham R. Robertson, Jacqueline Field, Bryan Goodwin, Sandra Bierach, Minh Tran, Anne Lehnert, and Christopher Liddle 42 Bcl-2 Down-Regulation Is a Novel Mechanism of Paclitaxel Resistance Cristiano Ferlini, Giuseppina Raspaglio, Simona Mozzetti, Mariagrazia Distefano, Flavia Filippetti, Enrica Martinelli, Gabriella Ferrandina, Daniela Gallo, Franco Oreste Ranelletti, and Giovanni Scambia 51 APETxl, a New Toxin from the Sea Anemone Anthopleura elegantissima, Blocks Voltage-Gated Human Ether-a-go-go-Related Gene Potassium Channels Sylvie Diochot, Erwann Loret, Thomas Bruhn, Ldszlo Beress, and Michel Lazdunski 59 Molecular Determinants of KCNQ1 Channel Block by a Benzodiazepine Guiscard Seebohm, Jun Chen, Nathalie Strutz, Chris Culberson, Christian Lerche, and Michael C. Sanguinetti 70 Positive Allosteric Modulator of the Human 5-HT2C Receptor Wha Bin Im, Christopher L. Chio, Glen L. Alberts, and Dae M. Dinh

78 1214 Anti-Inflammatory Activity of 15-Deoxy-A -PGJ2 and 2-Cyclopenten-l-one: Role of the Heat Shock Response Angela lanaro, Armando Ialenti, Pasquale Maffia, Paola Di Meglio, Massimo Di Rosa, and M. Gabriella Santoro 85 I Molecular Determination of Agouti-Related Protein Binding to Human Melanocortin-4 Receptor Yingkui Yang, Min Chen, Yumei Lai, Ira Gantz, Aydin Yagmurlu, Keith E. Georgeson, and Carroll M. Harmon

Pharmacological Characterization of the Human P2Y13 Receptor Frederic Marteau, Emmanuel Le Poul, David Communi, Didier Communi, Catherine Labouret, Pierre Savi, Jean-Marie Boeynaems, and Nathalie Suarez Gonzalez

104 Regulation of CYP2C11 by Dehydroepiandrosterone and Peroxisome Proliferators: Identification of the Negative Regulatory Region of the Gene Sharon L. Ripp, K. Cameron Falkner, Mary L. Pendleton, Viola Tamasi, and Russell A, Prough 113 Jesterone Dimer, a Synthetic Derivative of the Fungal Metabolite Jesterone, Blocks Activation of Transcription Factor Nuclear Factor KB by Inhibiting the Inhibitor of KB Kinase Mei-Chih Liang, Sujata Bardhan, Chaomin Li, Emily A. Pace, John A. Porco, Jr, and Thomas D. Gilmore 123 Corticotropin Induces the Expression of TREK-1 mRNA and K + Current in Adrenocortical Cells Judith A. Enyeart, Sanjay Danthi, and John J. Enyeart 132 [125I]A-312110, a Novel High-Affinity 1,4-Dihydropyridine ATP-sensitive K+ Channel Opener: Characterization and Pharmacology of Binding Rachel Davis-Taber, Eduardo J. Molinari, Robert J. Altenbach, Kristi L. Whiteaker, Char-Chang Shieh, Gary Rotert, Steven A. Buckner, John Malysz, Ivan Milicic, Jeffrey S. McDermott, Gary A. Gintant, Michael J. Coghlan, William A. Carroll, Victoria E. Scott, and Murali Gopalakrishnan 143 Phenobarbital Alters Hepatic Mrp2 Function by Direct and Indirect Interactions Nita J. Patel, Maciej J. Zamek-Gliszczynski, Peijin Zhang, Yong-Hae Han, Peter L. M. Jansen, Peter J. Meier, Bruno Stieger, and Kim L. R. Brouwer 154 Colchicine Down-Regulates Cytochrome P450 2B6, 2C8, 2C9, and 3A4 in Human Hepatocytes by Affecting Their Glucocorticoid Receptor-Mediated Regulation Zdenek Dvorak, Martin Modriansky, Lydiane Pichard-Garcia, Patrick Balaguer, Marie-Jose Vilarem, Jitka Ulrichovd, Patrick Maurel, and Jean-Marc Pascussi 160 Generation and Functional Characterization of Arylamine iV-Acetyltransferase Natl/Nat2 Double- Knockout Mice Kim S. Sugamori, Sharon Wong, Andrea Gaedigk, Violeta Yu, Hanan Abramovici, Richard Rozmahel, and Denis M. Grant 170 Interactions of Orthosteric and Allosteric Ligands with [3H]Dimethyl-W84 at the Common Allosteric Site of Muscarinic M2 Receptors Christian Trdnkle, Oliver Weyand, Uta Voigtldnder, Anita Mynett, Sebastian Lazareno, Nigel J. M. Birdsall, and Klaus Mohr 180 Editors' Note regarding "Mechanism of corticotropin-releasing factor type I receptor regulation by nonpeptide antagonists" 191

Correction to "Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2" 192 Correction to "Spatial approximation between a photolabile residue in position 13 of secretin and the amino terminus of the secretin receptor" 193