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A B Pharmacology Molecular A Publication of the American Society for Pharmacology and Experimental Therapeutics Volume 73 ■ Number 4 ■ April 2008 ■ ISSN 0026-895X
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PharmacologyMolecular
A Publication of the American Society for
Pharmacology and Experimental Therapeutics
Volume 73 ■ Number 4 ■ April 2008 ■ ISSN 0026-895X
zmo0040800SPC1.qxd 3/10/08 3:56 PM Page 1
ACCELERATED COMMUNICATION□S The RGS2 Gene Product from a Candidate Hypertension Allele Shows Decreased Plasma Membrane
Association and Inhibition of GqSteven Gu, Sam Tirgari, and Scott P. Heximer 1037
ARTICLESA Single Amino Acid Difference between Ether-a-go-go-Related Gene Channel Subtypes Determines
Differential Sensitivity to a Small Molecule ActivatorMatthew Perry and Michael C. Sanguinetti 1044
□S Rapamycin Inhibits Polyglutamine Aggregation Independently of Autophagy by Reducing ProteinSynthesisMatthew A. King, Sarah Hands, Farida Hafiz, Noboru Mizushima, Aviva M. Tolkovsky, andAndreas Wyttenbach 1052
Development of an Aryl Hydrocarbon Receptor Antagonist Using the Proteolysis-Targeting ChimericMolecules Approach: A Potential Tool for ChemopreventionDinesh Puppala, Hyosung Lee, Kyung Bo Kim, and Hollie I. Swanson 1064
Madin-Darby Canine Kidney II Cells: A Pharmacologically Validated System for NPC1L1-MediatedCholesterol UptakeAdam B. Weinglass, Martin G. Kohler, Emmanuel O. Nketiah, Jessica Liu, William Schmalhofer,Anu Thomas, Brande Williams, Lindsey Beers, Lauren Smith, Mike Hafey, Kelly Bleasby,Joseph Leone, Yui Sing Tang, Matthew Braun, Feroze Ujjainwalla, Margaret E. McCann,Gregory J. Kaczorowski, and Maria L. Garcia 1072
□S Salicylate Alters the Expression of Calcium Response Transcription Factor 1 in the Cochlea:Implications for Brain-Derived Neurotrophic Factor Transcriptional RegulationWibke Singer, Rama Panford-Walsh, Dirk Watermann, Oliver Hendrich, Ulrike Zimmermann,Iris Kopschall, Karin Rohbock, and Marlies Knipper 1085
□S Wide Turn Diversity in Protein Transmembrane Helices Implications for G-Protein-Coupled Receptorand Other Polytopic Membrane Protein Structure and FunctionR. Peter Riek, Angela A. Finch, Gillian E. Begg, and Robert M. Graham 1092
MOLECULARPHARMACOLOGY
April 2008 Volume 73 Number 4 http://molpharm.aspetjournals.org ISSN 0026-895X
Molecular Pharmacology (ISSN 0026-895X) is published monthly(two volumes per year beginning in January and July) by the Amer-ican Society for Pharmacology and Experimental Therapeutics, 9650Rockville Pike, Bethesda, MD 20814-3995; e-mail: [email protected];Web site: http://www.aspet.org. Periodicals postage paid at Bethesda,MD and at additional mailing offices. POSTMASTER: Send addresschanges to Molecular Pharmacology, 9650 Rockville Pike, Bethesda,MD 20814-3995. Subscription rates: U.S.: $647.00 for institutionsand $264.00 for non-ASPET members. Outside the U.S.: $734.00for institutions and $351.00 for non-ASPET members. Single copy:
$59.00. GST Tax Number for Canadian subscribers: BN:13489 2330RT. Indexed or abstracted by Biochemistry & Biophysics CitationIndex®, Biological Abstracts, BIOSIS Previews Database, CurrentAwareness in Biological Sciences, Current Contents®/Life Sciences,EMBASE/Excerpta Medica, Index Medicus, Medical DocumentationService®, Reference Update®, Research Alert®, Science CitationIndex®, SciSearch®, and SIIC Data Bases. Copyright © 2008 by theAmerican Society for Pharmacology and Experimental Therapeutics.All rights reserved. Printed in the U.S.A.
Dopamine and Ethanol Cause Translocation of �PKC Associated with �RACK: Cross-Talk betweencAMP-Dependent Protein Kinase A and Protein Kinase C Signaling PathwaysLina Yao, Peidong Fan, Zhan Jiang, Adrienne Gordon, Daria Mochly-Rosen, and Ivan Diamond 1105
PPP1R16A, The Membrane Subunit of Protein Phosphatase 1�, Signals Nuclear Translocation of theNuclear Receptor Constitutive Active/Androstane ReceptorTatsuya Sueyoshi, Rick Moore, Junko Sugatani, Yonehiro Matsumura, and Masahiko Negishi 1113
□S Improvement of Cyclophosphamide Activation by CYP2B6 Mutants: From in Silico to ex VivoThien-An Nguyen, Marina Tychopoulos, Florence Bichat, Clothilde Zimmermann,Jean-Pierre Flinois, Monique Diry, Emelie Ahlberg, Marcel Delaforge, Laurent Corcos,Philippe Beaune, Patrick Dansette, Francois Andre, and Isabelle de Waziers 1122
Effects of High-Affinity Inhibitors on Partial Reactions, Charge Movements, and Conformational Statesof the Ca2� Transport ATPase (Sarco-Endoplasmic Reticulum Ca2� ATPase)Francesco Tadini-Buoninsegni, Gianluca Bartolommei, Maria Rosa Moncelli, Daniel M. Tal,David Lewis, and Giuseppe Inesi 1134
Labeling of Dopamine Transporter Transmembrane Domain 1 with the Tropane Ligand N-[4-(4-Azido-3-[125I]iodophenyl)butyl]-2�-carbomethoxy-3�-(4-chlorophenyl)tropane Implicates Proximity ofCocaine and Substrate Active SitesM. Laura Parnas, Jon D. Gaffaney, Mu Fa Zou, John R. Lever, Amy Hauck Newman, andRoxanne A. Vaughan 1141
Organic Anion Transporter 2 (SLC22A7) Is a Facilitative Transporter of cGMPCheryl D. Cropp, Takafumi Komori, James E. Shima, Thomas J. Urban, Sook Wah Yee,Swati S. More, and Kathleen M. Giacomini 1151
□S Structural Basis for Ether-a-go-go-Related Gene K� Channel Subtype-Dependent Activation byNiflumic AcidDavid Fernandez, John Sargent, Frank B. Sachse, and Michael C. Sanguinetti 1159
OSU-03012 Stimulates PKR-Like Endoplasmic Reticulum-Dependent Increases in 70-kDa Heat ShockProtein Expression, Attenuating Its Lethal Actions in Transformed CellsMargaret A. Park, Adly Yacoub, Mohammed Rahmani, Guo Zhang, Lori Hart, Michael P. Hagan,Stuart K. Calderwood, Michael Y. Sherman, Costas Koumenis, Sarah Spiegel, Ching-Shih Chen,Martin Graf, David T. Curiel, Paul B. Fisher, Steven Grant, and Paul Dent 1168
Arachidonic Acid Activates Kir2.3 Channels by Enhancing Channel–Phosphatidyl-inositol 4,5-bisphosphate InteractionsChuan Wang, Uyenlinh L. Mirshahi, Boyi Liu, Zhanfeng Jia, Tooraj Mirshahi, and Hailin Zhang 1185
�2 Subunit Specificity of Cyclothiazide Inhibition on Glycine ReceptorsXiao-Bing Zhang, Guang-Chun Sun, Lu-Ying Liu, Fang Yu, and Tian-Le Xu 1195
Enhanced Excitation-Coupled Calcium Entry in Myotubes Expressing Malignant HyperthermiaMutation R163C Is Attenuated by DantroleneGennady Cherednichenko, Chris W. Ward, Wei Feng, Elaine Cabrales, Luke Michaelson,Montserrat Samso, Jose R. Lopez, Paul D. Allen, and Isaac N. Pessah 1203
A Novel Assay of Gi/o-Linked G Protein-Coupled Receptor Coupling to Potassium Channels ProvidesNew Insights into the Pharmacology of the Group III Metabotropic Glutamate ReceptorsColleen M. Niswender, Kari A. Johnson, Qingwei Luo, Jennifer E. Ayala, Caroline Kim,P. Jeffrey Conn, and C. David Weaver 1213
Activation of TRPA1 by Farnesyl Thiosalicylic AcidMichael Maher, Hong Ao, Tue Banke, Nadia Nasser, Nyan-Tsz Wu, J. Guy Breitenbucher,Sandra R. Chaplan, and Alan D. Wickenden 1225
□S Pharmacological and Kinetic Characterization of Adrenomedullin 1 and Calcitonin Gene-RelatedPeptide 1 Receptor Reporter Cell LinesFrank Wunder, Annegret Rebmann, Andreas Geerts, and Bernd Kalthof 1235
BYK191023 (2-[2-(4-Methoxy-pyridin-2-yl)-ethyl]-3H-imidazo[4,5-b]pyridine) Is an NADPH- and Time-Dependent Irreversible Inhibitor of Inducible Nitric-Oxide SynthaseMauro Tiso, Andreas Strub, Christian Hesslinger, Claire T. Kenney, Rainer Boer, andDennis J. Stuehr 1244
Modulation of Na�-Ca2� Exchanger Expression by Immunosuppressive Drugs Is Isoform-SpecificBenayahu Elbaz, Ariella Alperovitch, Michael M. Gottesman, Chava Kimchi-Sarfaty, andHannah Rahamimoff 1254
□S Anti-HIV Activity and Resistance Profile of the CXC Chemokine Receptor 4 Antagonist POL3026Gemma Moncunill, Mercedes Armand-Ugon, Imma Clotet-Codina, Eduardo Pauls, Ester Ballana,Anuska Llano, Barbara Romagnoli, Jan W. Vrijbloed, Frank O. Gombert, Bonaventura Clotet,Steve De Marco, and Jose A. Este 1264
□S Role of Lysine 411 in Substrate Carboxyl Group Binding to the Human Reduced Folate Carrier, asDetermined by Site-Directed Mutagenesis and Affinity InhibitionYijun Deng, Zhanjun Hou, Lei Wang, Christina Cherian, Jianmei Wu, Aleem Gangjee, andLarry H. Matherly 1274
Regulatory Cross-Talk between Drug Metabolism and Lipid Homeostasis: Constitutive AndrostaneReceptor and Pregnane X Receptor Increase Insig-1 ExpressionAdrian Roth, Renate Looser, Michel Kaufmann, Sharon M. Blattler, Franck Rencurel,Wendong Huang, David D. Moore, and Urs A. Meyer 1282
Molecular Mechanisms Underlying the Synergistic Interaction of Erlotinib, an Epidermal GrowthFactor Receptor Tyrosine Kinase Inhibitor, with the Multitargeted Antifolate Pemetrexed in Non–Small-Cell Lung Cancer CellsElisa Giovannetti, Clara Lemos, Christina Tekle, Kees Smid, Sara Nannizzi, Jose A. Rodriguez,Simona Ricciardi, Romano Danesi, Giuseppe Giaccone, and Godefridus J. Peters 1290
□S Agonist-Specific Regulation of �-Opioid Receptor Desensitization and Recovery from DesensitizationMichael S. Virk and John T. Williams 1301
Benzoxathiole Derivative Blocks Lipopolysaccharide-Induced Nuclear Factor-�B Activation and NuclearFactor-�B-Regulated Gene Transcription through Inactivating Inhibitory �B Kinase �Byung Hak Kim, Eunmiri Roh, Hwa Young Lee, In-Jeong Lee, Byeongwoo Ahn, Sang-Hun Jung,Heesoon Lee, Sang-Bae Han, and Youngsoo Kim 1309
□S Agonist-Promoted Lys63-Linked Polyubiquitination of the Human �-Opioid Receptor Is Involved inReceptor Down-RegulationJian-Guo Li, Dale S. Haines, and Lee-Yuan Liu-Chen 1319
ERRATUMCorrection to “Endocrine Regulation of Gender-Divergent Mouse Organic Anion-Transporting
Polypeptide (Oatp) Expression” 1331
□S Supplemental material is available online at http://molpharm.aspetjournals.org.
About the cover: CYP2B6 active site showing residues potentially close to CPA (in blue) docked inside. See the article by Nguyen etal. on page 1122 of this issue.
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