Probing Receptor Structure/Function with Chimeric G-Protein-Coupled Receptors

MOLECULAR PHARMACOLOGY June 2004 Volume 65 Number 6 http://molpharm.aspetjournals.org ISSN 0026-895X

MINIREVIEW Probing Receptor Structure/Function with Chimeric G-Protein-Coupled Receptors Dezhong Yin, Shai Gavi, Hsien-yu Wang, and Craig C. Malbon 1323 PERSPECTIVE Getting Past the Asterisk: the Subunit Composition of Presynaptic Nicotinic Receptors That Modulate Striatal Dopamine Release ID Charles W. Luetje -; 1333 ARTICLES Discovery of Novel Selective Inhibitors of Human Intestinal Carboxylesterase for the Amelioration of Irinotecan-Induced Diarrhea: Synthesis, Quantitative Structure-Activity Relationship Analysis, and Biological Activity Randy M. Wadkins, Janice L Hyatt, Kyoung Jin P. Yoon, Christopher L. Morton, Richard E. Lee, Komath Damodaran, Paul Beroza, Mary K. Banks, and Philip M. Potter 1336

Herbimycin A Abrogates Nuclear Factor-KB Activation by Interacting Preferentially with the IKB Kinase /3 Subunit Shinichi Ogino, Kazuhiro Tsuruma, Takashi Uehara, and Yasuyuki Nomura 1344 Insulin Activates Native and Recombinant Large Conductance Ca 2+-Activated Potassium Channels via a Mitogen-Activated Protein Kinase-Dependent Process Dervla O'Malley and Jenni Harvey 1352 Kvl.3-Blocking 5-Phenylalkoxypsoralens: A New Class of Immunomodulators Julia Vennekamp, Heike Wulff, Christine Beeton, Peter A. Calabresi, Stephan Grissmer, Wolfram Hansel, and K. George Chandy 1364 Mutations of Charged Amino Acids in or near the Transmembrane Helices of the Second Membrane Spanning Domain Differentially Affect the Substrate Specificity and Transport Activity of the Multidrug Resistance Protein MRP1 (ABCC1) Anass Haimeur, Gwenaelle Conseil, Roger G. Deeley, and Susan P.C. Cole 1375 Adenosine Triphosphate Acts as Both a Competitive Antagonist and a Positive Allosteric Modulator at Recombinant iV-Methyl-d-aspartate Receptors Anna Kloda, John D. Clements, Richard J. Lewis, and David J. Adams 1386 The Constitutive Active/Androstane Receptor Regulates Phenytoin Induction of Cyp2c29 Jonathan P. Jackson, Stephen S. Ferguson, Rick Moore, Masahiko Negishi, and Joyce A. Goldstein 1397 Interaction of Heterogeneous Nuclear Ribonucleoprotein Al with Cytochrome P450 2A6 mRNA: Implications for Post-Transcriptional Regulation of the CYP2A6 Gene Kyle Christian, Matti Lang, Patrick Maurel, and Francoise Raffalli-Mathieu 1405

Capsaicin Potentiates Wild-Type and Mutant Cystic Fibrosis Transmembrane Conductance Regulator Chloride-Channel Currents Tomohiko Ai, Silvia G. Bompadre, Xiaohui Wang, Shenghui Hu, Min Li, and Tzyh-Chang Hwang 1415

Signal Transducer and Activator of Transcription 3 Activation by the S-Opioid Receptor via Ga 14 Involves Multiple Intermediates Rico K. H. Lo and Yung H. Wong 1427 Down-Regulation of Soluble Guanylyl Cyclase Expression by Cyclic AMP Is Mediated by mRNA- Stabilizing Protein HuR Stephan Klb'ss, Rashi Srivastava, and Alexander Miilsch 1440 Transmembrane Domains I and II of the 7-Aminobutyric Acid Transporter GAT-4 Contain Molecular Determinants of Substrate Specificity Nir Melamed and Baruch I. Kanner 1452 Adenosine Receptor, Protein Kinase G, and p38 Mitogen-Activated Protein Kinase-Dependent Up- Regulation of Serotonin Transporters Involves Both Transporter Trafficking and Activation Chong-Bin Zhu, William A. Hewlett, Igor Feoktistov, Halo Biaggioni, and Randy D. Blakely 1462 Ceramide Negatively Regulates Glutathione S-transferase Gene Transactivation via Repression of Hepatic Nuclear Factor-1 That Is Degraded by the Ubiquitin Proteasome System I-Na Park, 11 Je Cho, and Sang Geon Kim 1475 High-Affinity Interaction of Tyrosine Kinase Inhibitors with the ABCG2 Multidrug Transporter Csilla Ozvegy-Laczka, Tamds Hegedus, Gyorgy Vdrady, Olga Ujhelly, John D. Schuetz, Andrds Vdradi, Gyorgy Keri, Ldszlo Orfi, Katalin Nemet, and Baldzs Sarkadi 1485 DNA Damage-Processing Pathways Involved in the Eukaryotic Cellular Response to Anticancer DNA Cross-Linking Drugs Vladimir Beljanski, Luigi G. Marzilli, and Paul W. Doetsch 1496 Activation of Cyclic AMP-Dependent Protein Kinase Inhibits the Desensitization and Internalization of Metabotropic Glutamate Receptors la and lb Stuart J. Mundell, Giordano Pula, Julia C. A. More,

Eamonn Kelly 1507 David E. Jane, Peter J, Roberts, and Eamonn Kelly Alternative Processing Events in Human FMO Genes Virginie Lattard, Jun Zhang, and John R. Cashman 1517 Subunit Composition and Pharmacology of Two Classes of Striatal Presynaptic Nicotinic Acetylcholine Receptors Mediating Dopamine Release in Mice Outi Salminen, Karen L. Murphy, J. Michael Mclntosh, John Drago, Michael J. Marks, Allan C. Collins, and Sharon R. Grady 1526 Function of the ABC Signature Sequences in the Human Multidrug Resistance Protein 1 Xiao-Qin Ren, Tatsuhiko Furukawa, Misako Haraguchi, Tomoyuki Sumizawa, Shunji Aoki, Motomasa Kobayashi, Shin-ichi Akiyama 1536