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
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
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
Allosteric Site on Muscarinic Acetylcholine Receptors: Identification of Two Amino Acids in the
Muscarinic M2 Receptor That Account Entirely for the M 2/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
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
1
5
11
21
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
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
85
94
Pharmacological Characterization of the Human P2Y 13 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 K B by Inhibiting the Inhibitor of K B Kinase
Mei-Chih Liang, Sujata Bardhan, Chaomin Li, Emily A. Pace, John A. Porco, Jr, and
Thomas D. Gilmore
Corticotropin Induces the Expression of TREK-1 mRNA and K + Current in Adrenocortical Cells
Judith A. Enyeart, Sanjay Danthi, and John J. Enyeart
125
[ I]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
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
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
Generation and Functional Characterization of Arylamine iV-Acetyltransferase Natl/Nat2 DoubleKnockout Mice
Kim S. Sugamori, Sharon Wong, Andrea Gaedigk, Violeta Yu, Hanan Abramovici,
Richard Rozmahel, and Denis M. Grant
123
132
143
154
160
170
3
Interactions of Orthosteric and Allosteric Ligands with [ H]Dimethyl-W84 at the Common Allosteric
Site of Muscarinic M 2 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 EP 4 mediates the bone anabolic effects of PGE 2"
192
Correction to "Spatial approximation between a photolabile residue in position 13 of secretin and the
amino terminus of the secretin receptor"
193