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Pharmacology Molecular A Publication of the American Society for Pharmacology and Experimental Therapeutics Volume 73 ■ Number 2 ■ February 2008 ■ ISSN 0026-895X
PharmacologyMolecular
A Publication of the American Society for
Pharmacology and Experimental Therapeutics
Volume 73 ■ Number 2 ■ February 2008 ■ ISSN 0026-895X
zmo0020800SPC1.qxd 1/15/08 8:28 AM Page 1
PERSPECTIVERevoking the Privilege: Targeting HER2 in the Central Nervous System
Joseph N. Contessa and Daniel A. Hamstra 271
ACCELERATED COMMUNICATIONProstaglandin-Induced Activation of Nociceptive Neurons via Direct Interaction with Transient
Receptor Potential A1 (TRPA1)Thomas E. Taylor-Clark, Bradley J. Undem, Donald W. MacGlashan, Jr., Srinivas Ghatta,Michael J. Carr, and M. Allen McAlexander 274
ARTICLESCortical Glutamatergic Neurons Mediate the Motor Sedative Action of Diazepam
A. Zeller, F. Crestani, I. Camenisch, T. Iwasato, S. Itohara, J. M. Fritschy, and U. Rudolph 282
Distinct Phosphorylation Sites in the SST2A Somatostatin Receptor Control Internalization,Desensitization, and Arrestin BindingQ. Liu, D. A. Dewi, W. Liu, M. S. Bee, and A. Schonbrunn 292
Conformational Flexibility of Helix VI Is Essential for Substrate Permeation of the Human ApicalSodium-Dependent Bile Acid TransporterNaissan Hussainzada, Akash Khandewal, and Peter W. Swaan 305
Anandamide Inhibition of 5-HT3A Receptors Varies with Receptor Density and DesensitizationWei Xiong, Masako Hosoi, Bon-Nyeo Koo, and Li Zhang 314
□S Peroxisome Proliferator-Activated Receptor-� Contributes to the Anti-Inflammatory Activity ofGlucocorticoidsSalvatore Cuzzocrea, Stefano Bruscoli, Emanuela Mazzon, Concetta Crisafulli, Valerio Donato,Rosanna Di Paola, Enrico Velardi, Emanuela Esposito, Giuseppe Nocentini, and Carlo Riccardi 323
Cellular and in Vivo Activity of JNJ-28871063, A Nonquinazoline Pan-ErbB Kinase Inhibitor ThatCrosses the Blood-Brain Barrier and Displays Efficacy against Intracranial TumorsStuart L. Emanuel, Terry V. Hughes, Mary Adams, Catherine A. Rugg, Angel Fuentes-Pesquera,Peter J. Connolly, Niranjan Pandey, Sandra Moreno-Mazza, Jeannene Butler, Virna Borowski,Steven A. Middleton, Robert H. Gruninger, Jennifer R. Story, Cheryl Napier, Beth Hollister, andLee M. Greenberger 338
MOLECULARPHARMACOLOGY
February 2008 Volume 73 Number 2 http://molpharm.aspetjournals.org ISSN 0026-895X
The symbols in the table of contents identify articles discussed in the Perspective.
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.
□S Characterization of G-Protein Coupled Receptor Kinase Interaction with the Neurokinin-1 ReceptorUsing Bioluminescence Resonance Energy TransferRasmus Jorgensen, Nicholas D. Holliday, Jakob L. Hansen, Milka Vrecl, Anders Heding,Thue W. Schwartz, and Christian E. Elling 349
A Novel Actin-Binding Domain on Slo1 Calcium-Activated Potassium Channels Is Necessary for TheirExpression in the Plasma MembraneShengwei Zou, Smita Jha, Eun Young Kim, and Stuart E. Dryer 359
The �1 Subunit of L-Type Voltage-Gated Ca2� Channels Independently Binds to and Inhibits theGating of Large-Conductance Ca2�-Activated K� ChannelsShengwei Zou, Smita Jha, Eun Young Kim, and Stuart E. Dryer 369
Functional Characterization of a Nucleoside-Derived Drug Transporter Variant (hCNT3C602R) ShowingAltered Sodium-Binding CapacityEkaitz Errasti-Murugarren, Pedro Cano-Soldado, Marcal Pastor-Anglada, and Fco Javier Casado 379
Repression of Aryl Hydrocarbon Receptor (AHR) Signaling by AHR Repressor: Role of DNA Bindingand Competition for AHR Nuclear TranslocatorBrad R. Evans, Sibel I. Karchner, Lenka L. Allan, Richard S. Pollenz, Robert L. Tanguay,Matthew J. Jenny, David H. Sherr, and Mark E. Hahn 387
Curcumin Protects the Rat Liver from CCl4-Caused Injury and Fibrogenesis by Attenuating OxidativeStress and Suppressing InflammationYumei Fu, Shizhong Zheng, Jianguo Lin, Jan Ryerse, and Anping Chen 399
Small Molecule Disruption of G Protein �� Subunit Signaling Inhibits Neutrophil Chemotaxis andInflammationD. M. Lehmann, A. M. P. B. Seneviratne, and A. V. Smrcka 410
□S BubR1 Is Required for a Sustained Mitotic Spindle Checkpoint Arrest in Human Cancer Cells Treatedwith Tubulin-Targeting Pyrrolo-1,5-BenzoxazepinesLisa M. Greene, Giuseppe Campiani, Mark Lawler, D. Clive Williams, and Daniela M. Zisterer 419
Role of Extracellular Domain Dimerization in Agonist-Induced Activation of Natriuretic PeptideReceptor AMarie Parat, Normand McNicoll, Brian Wilkes, Alain Fournier, and Andre De Lean 431
Inhibition of Human Neutrophil Chemotaxis by Endogenous Cannabinoids and Phytocannabinoids:Evidence for a Site Distinct from CB1 and CB2Douglas McHugh, Carolyn Tanner, Raphael Mechoulam, Roger G. Pertwee, and Ruth A. Ross 441
Dexamethasone-Mediated Up-Regulation of Human CYP2A6 Involves the Glucocorticoid Receptor andIncreased Binding of Hepatic Nuclear Factor 4� to the Proximal PromoterTania Onica, Kathleen Nichols, Meghan Larin, Lorraine Ng, Ann Maslen, Zdenek Dvorak,Jean-Marc Pascussi, Marie-Josee Vilarem, Patrick Maurel, and Gordon M. Kirby 451
Transport of Cisplatin by the Copper Efflux Transporter ATP7BRoohangiz Safaei, Shinji Otani, Barrett J. Larson, Michael L. Rasmussen, and Stephen B. Howell 461
Cloning and Functional Expression of a Novel Gi Protein-Coupled Receptor for Adenine from Mouse BrainIvar von Kugelgen, Anke C. Schiedel, Kristina Hoffmann, Bernt B. A. Alsdorf, Aliaa Abdelrahman,and Christa E. Muller 469
Structural Analog of Sildenafil Identified as a Novel Corrector of the F508del-CFTR Trafficking DefectRenaud Robert, Graeme W. Carlile, Catalin Pavel, Na Liu, Suzana M. Anjos, Jie Liao, Yishan Luo,Donglei Zhang, David Y. Thomas, and John W. Hanrahan 478
Reduced Expression of DNA Topoisomerase I in SF295 Human Glioblastoma Cells Selected forResistance to Homocamptothecin and DiflomotecanZhiyong Liao, Robert W. Robey, Josee Guirouilh-Barbat, Kenneth K. W. To, Orsolya Polgar,Susan E. Bates, and Yves Pommier 490
Impact of Targeting the Adenine- and Uracil-Rich Element of bcl-2 mRNA with Oligoribonucleotides onApoptosis, Cell Cycle, and Neuronal Differentiation in SHSY-5Y CellsLaura Papucci, Ewa Witort, Anna Maria Bevilacqua, Martino Donnini, Matteo Lulli,Elisabetta Borchi, Khalid S. A. Khabar, Alessio Tempestini, Andrea Lapucci, Nicola Schiavone,Angelo Nicolin, and Sergio Capaccioli 498
A Peroxisome Proliferator-Activated Receptor �-Retinoid X Receptor Heterodimer Physically Interactswith the Transcriptional Activator PAX6 to Inhibit Glucagon Gene TranscriptionRalph Kratzner, Florian Frohlich, Katrin Lepler, Michaela Schroder, Katharina Roher,Corinna Dickel, Mladen V. Tzvetkov, Thomas Quentin, Elke Oetjen, and Willhart Knepel 509
[3H]Org 43553, the First Low-Molecular-Weight Agonistic and Allosteric Radioligand for the HumanLuteinizing Hormone ReceptorLaura H. Heitman, Julia Oosterom, Kimberly M. Bonger, Cornelis M. Timmers,Peter H. G. Wiegerinck, and Adriaan P. IJzerman 518
□S Multiple Binding Sites for Substrates and Modulators of Semicarbazide-Sensitive Amine Oxidases:Kinetic ConsequencesAndrew Holt, David J. Smith, Laura Cendron, Giuseppe Zanotti, Adelio Rigo, andMaria Luisa Di Paolo 525
□S Functional Characterization of Bone Morphogenetic Protein Binding Sites and Smad1/5 Activation inHuman Vascular CellsPaul D. Upton, Lu Long, Richard C. Trembath, and Nicholas W. Morrell 539
Methyl 2-Cyano-3,11-dioxo-18�-olean-1,12-dien-30-oate Is a Peroxisome Proliferator-ActivatedReceptor-� Agonist That Induces Receptor-Independent Apoptosis in LNCaP Prostate Cancer CellsSabitha Papineni, Sudhakar Chintharlapalli, and Stephen Safe 553
Mitogenic Effects of Cytokines on Smooth Muscle Are Critically Dependent on Protein Kinase A andAre Unmasked by Steroids and Cyclooxygenase InhibitorsAnna M. Misior, Huandong Yan, Rodolfo M. Pascual, Deepak A. Deshpande, Reynold A. Panettieri,and Raymond B. Penn 566
□S 3-Methylcholanthrene Displays Dual Effects on Estrogen Receptor (ER) � and ER� Signaling in a Cell-Type Specific FashionElin Swedenborg, Joelle Ruegg, Anne Hillenweck, Stefan Rehnmark, Malin Hedengran Faulds,Daniel Zalko, Ingemar Pongratz, and Katarina Pettersson 575
Regulation of Lysophosphatidic Acid Receptor Expression and Function in Human Synoviocytes:Implications for Rheumatoid Arthritis?Chenqi Zhao, Maria J. Fernandes, Glenn D. Prestwich, Melanie Turgeon, John Di Battista,Timothy Clair, Patrice E. Poubelle, and Sylvain G. Bourgoin 587
Efavirenz Accelerates HIV-1 Reverse Transcriptase Ribonuclease H Cleavage, Leading to DiminishedZidovudine ExcisionJessica Radzio and Nicolas Sluis-Cremer 601
Regulation of Human 3�-Hydroxysteroid Dehydrogenase (AKR1C4) Expression by the Liver X Receptor �Keith R. Stayrook, Pamela M. Rogers, Rajesh S. Savkur, Yongjun Wang, Chen Su, Gabor Varga,Xin Bu, Tao Wei, Sunil Nagpal, Xiaole Shirley Liu, and Thomas P. Burris 607
□S Supplemental material is available online at http://molpharm.aspetjournals.org.
About the cover: Region- and cell type-specific loss of �1 subunit IR in forebrain-specific �1�/� mice. See the article by Zeller et al.,on page 282 of this issue.
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