Front Matter - Molecular Pharmacology

Volume 73
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Number 2
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February 2008
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ISSN 0026-895X
Molecular
Pharmacology
A Publication of the American Society for
Pharmacology and Experimental Therapeutics
MOLECULAR
PHARMACOLOGY
February 2008
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Volume 73
Number 2
http://molpharm.aspetjournals.org
ISSN 0026-895X
PERSPECTIVE
Revoking the Privilege: Targeting HER2 in the Central Nervous System
Joseph N. Contessa and Daniel A. Hamstra
271
ACCELERATED COMMUNICATION
Prostaglandin-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
ARTICLES
Cortical 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 Binding
Q. 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 Apical
Sodium-Dependent Bile Acid Transporter
Naissan Hussainzada, Akash Khandewal, and Peter W. Swaan
305
Anandamide Inhibition of 5-HT3A Receptors Varies with Receptor Density and Desensitization
Wei Xiong, Masako Hosoi, Bon-Nyeo Koo, and Li Zhang
314
Peroxisome Proliferator-Activated Receptor-␣ Contributes to the Anti-Inflammatory Activity of
Glucocorticoids
Salvatore 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 That
Crosses the Blood-Brain Barrier and Displays Efficacy against Intracranial Tumors
Stuart 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, and
Lee M. Greenberger
338
The
symbols in the table of contents identify articles discussed in the Perspective.
Molecular Pharmacology (ISSN 0026-895X) is published monthly
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RT. Indexed or abstracted by Biochemistry & Biophysics Citation
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All rights reserved. Printed in the U.S.A.
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Characterization of G-Protein Coupled Receptor Kinase Interaction with the Neurokinin-1 Receptor
Using Bioluminescence Resonance Energy Transfer
Rasmus 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 Their
Expression in the Plasma Membrane
Shengwei 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 the
Gating of Large-Conductance Ca2⫹-Activated K⫹ Channels
Shengwei Zou, Smita Jha, Eun Young Kim, and Stuart E. Dryer
369
Functional Characterization of a Nucleoside-Derived Drug Transporter Variant (hCNT3C602R) Showing
Altered Sodium-Binding Capacity
Ekaitz Errasti-Murugarren, Pedro Cano-Soldado, Marçal Pastor-Anglada, and Fco Javier Casado
379
Repression of Aryl Hydrocarbon Receptor (AHR) Signaling by AHR Repressor: Role of DNA Binding
and Competition for AHR Nuclear Translocator
Brad 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 Oxidative
Stress and Suppressing Inflammation
Yumei Fu, Shizhong Zheng, Jianguo Lin, Jan Ryerse, and Anping Chen
399
Small Molecule Disruption of G Protein ␤␥ Subunit Signaling Inhibits Neutrophil Chemotaxis and
Inflammation
D. M. Lehmann, A. M. P. B. Seneviratne, and A. V. Smrcka
410
BubR1 Is Required for a Sustained Mitotic Spindle Checkpoint Arrest in Human Cancer Cells Treated
with Tubulin-Targeting Pyrrolo-1,5-Benzoxazepines
Lisa 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 Peptide
Receptor A
Marie Parat, Normand McNicoll, Brian Wilkes, Alain Fournier, and André De Léan
431
Inhibition of Human Neutrophil Chemotaxis by Endogenous Cannabinoids and Phytocannabinoids:
Evidence for a Site Distinct from CB1 and CB2
Douglas McHugh, Carolyn Tanner, Raphael Mechoulam, Roger G. Pertwee, and Ruth A. Ross
441
Dexamethasone-Mediated Up-Regulation of Human CYP2A6 Involves the Glucocorticoid Receptor and
Increased Binding of Hepatic Nuclear Factor 4␣ to the Proximal Promoter
Tania Onica, Kathleen Nichols, Meghan Larin, Lorraine Ng, Ann Maslen, Zdenek Dvorak,
Jean-Marc Pascussi, Marie-Josée Vilarem, Patrick Maurel, and Gordon M. Kirby
451
Transport of Cisplatin by the Copper Efflux Transporter ATP7B
Roohangiz 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 Brain
Ivar von Kügelgen, Anke C. Schiedel, Kristina Hoffmann, Bernt B. A. Alsdorf, Aliaa Abdelrahman,
and Christa E. Müller
469
Structural Analog of Sildenafil Identified as a Novel Corrector of the F508del-CFTR Trafficking Defect
Renaud 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 for
Resistance to Homocamptothecin and Diflomotecan
Zhiyong Liao, Robert W. Robey, Josée Guirouilh-Barbat, Kenneth K. W. To, Orsolya Polgar,
Susan E. Bates, and Yves Pommier
490
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Impact of Targeting the Adenine- and Uracil-Rich Element of bcl-2 mRNA with Oligoribonucleotides on
Apoptosis, Cell Cycle, and Neuronal Differentiation in SHSY-5Y Cells
Laura 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 Interacts
with the Transcriptional Activator PAX6 to Inhibit Glucagon Gene Transcription
Ralph Krätzner, Florian Fröhlich, Katrin Lepler, Michaela Schröder, Katharina Röher,
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 Human
Luteinizing Hormone Receptor
Laura H. Heitman, Julia Oosterom, Kimberly M. Bonger, Cornelis M. Timmers,
Peter H. G. Wiegerinck, and Adriaan P. IJzerman
518
Multiple Binding Sites for Substrates and Modulators of Semicarbazide-Sensitive Amine Oxidases:
Kinetic Consequences
Andrew Holt, David J. Smith, Laura Cendron, Giuseppe Zanotti, Adelio Rigo, and
Maria Luisa Di Paolo
525
Functional Characterization of Bone Morphogenetic Protein Binding Sites and Smad1/5 Activation in
Human Vascular Cells
Paul 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-Activated
Receptor-␥ Agonist That Induces Receptor-Independent Apoptosis in LNCaP Prostate Cancer Cells
Sabitha Papineni, Sudhakar Chintharlapalli, and Stephen Safe
553
Mitogenic Effects of Cytokines on Smooth Muscle Are Critically Dependent on Protein Kinase A and
Are Unmasked by Steroids and Cyclooxygenase Inhibitors
Anna M. Misior, Huandong Yan, Rodolfo M. Pascual, Deepak A. Deshpande, Reynold A. Panettieri,
and Raymond B. Penn
566
3-Methylcholanthrene Displays Dual Effects on Estrogen Receptor (ER) ␣ and ER␤ Signaling in a CellType Specific Fashion
Elin Swedenborg, Joëlle Rüegg, 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, Mélanie 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 Diminished
Zidovudine Excision
Jessica 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
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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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