Download 73_06_2008

MOLECULAR
PHARMACOLOGY
June 2008
Volume 73
Number 6
http://molpharm.aspetjournals.org
ISSN 0026-895X
PERSPECTIVES
Making the T-Type Even Tinier: Corticotropin-Releasing Factor-Mediated Inhibition of Low-VoltageActivated Calcium Channel Activity HO
Diego L. Varela, Tamara Hermosilla, and Gerald W. Zamponi
1589
Refining Insights into High-Affinity Drug Binding to the Human Ether-a-go-go-Related Gene
Potassium Channel <^
Jules C. Hancox and Andrew F. James
1592
ARTICLES
Activation of Corticotropin-Releasing Factor Receptor 1 Selectively Inhibits Ca v3.2 T-Type Calcium
Channels
Jin Tao, Michael E. Hildebrand, Ping Liao, Mui Cheng Liang, Gregory Tan, Shengnan Li,
Terrance P. Snutch, and Tuck Wah Soong
1596
Glucocorticoid-Induced Tumor Necrosis Factor Receptor-Related (GITR)-Fc Fusion Protein Inhibits GITR
Triggering and Protects from the Inflammatory Response after Spinal Cord Injury
Giuseppe Nocentini, Salvatore Cuzzocrea, Tiziana Genovese, Rodolfo Bianchini, Emanuela Mazzon,
Simona Ronchetti, Emanuela Esposito, Di Paola Rosanna, Placido Bramanti, and Carlo Riccardi
1610
Protease-Activated Receptor-1 Mediates Thrombin-Induced Persistent Sodium Current in Human
Cardiomyocytes
Caroline Pinet, Vincent Algalarrondo, Sylvie Sablayrolles, Bruno Le Grand, Christophe Pignier,
Didier Cussac, Michel Perez, Stephane N. Hatem, and Alain Coulombe
1622
Combined Targeting of Epidermal Growth Factor Receptor, Signal Transducer and Activator of
Transcription-3, and Bcl-X L Enhances Antitumor Effects in Squamous Cell Carcinoma of the Head
and Neck
Amanda L. Boehm, Malabika Sen, Raja Seethala, William E. Gooding, Maria Freilino,
Silvia Man Yan Wong, Shaomeng Wang, Daniel E. Johnson, and Jennifer Rubin Grandis
1632
Topological Mapping of the Asymmetric Drug Binding to the Human Ether-a-go-go-Related Gene E
Product (HERG) Potassium Channel by Use of Tandem Dimers
Toshihiko Myokai, Sunghi Ryu, Hirofumi Shimizu, and Shigetoshi Oiki
1643
The Nuclear Factor-KB Pathway Regulates Cytochrome P450 3A4 Protein Stability
R. C. Zangar, N. Bollinger, S. Verma, N. J. Karin, and Y. Lu
1652
A Role for Leull8 of Loop E in Agonist Binding to the a 7 Nicotinic Acetylcholine Receptor Shiva Amiri,
Masaru Shimomura, Ranjit Vijayan, Hisashi Nishiwaki, Miki Akamatsu, Kazuhiko Matsuda, Andrew K.
Jones, Mark S. P. Sansom, Philip C. Biggin, and David B. Sattelle
1659
] Multipathway Model Enables Prediction of Kinase Inhibitor Cross-Talk Effects on Migration of Her2Overexpressing Mammary Epithelial Cells
Neil Kumar, Raffi Afeyan, Hyung-Do Kim, and Douglas A. Lauffenburger
1668
Inhibition of e-Myc Down-Regulation by Sustained Extracellular Signal-Regulated Kinase Activation
Prevents the Antimetabolite Methotrexate- and Gemcitabine-Induced Differentiation in NonSmall-Cell Lung Cancer Cells
Jordi M. Serra, Antonio Gutierrez, Regina Alemany, Maria Navarro, Teresa Ros, Carlos Saus,
Jordi Gines, Antonia Sampol, Juan Carlos Amat, Lorenzo Serra-Moises, Javier Martin,
Antonio Galmes, Oliver Vb'gler, and Joan Besalduch
1679
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A cAMP-Dependent, Protein Kinase A-Independent Signaling Pathway Mediating Neuritogenesis
through Egrl in PC12 Cells
Aurelia Ravni, David Vaudry, Matthew J. Gerdin, Maribeth V. Eiden, Anthony Falluel -Morel,
Bruno J. Gonzalez, Hubert Vaudry, and Lee E. Eiden
1688
Probing the Binding Sites and Mechanisms of Action of Two Human Ether- a -go-go -Related Gene
Channel Activators, l,3-bis-(2-Hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) and 2-[2-(3,4Dichloro-phenyl)-2,3-dihydro-lH-isoindol-5-ylamino]-nicotinic acid (PD307243)
Xulin Xu, Maurizio Recanatini, Marinella Roberti, and Gea-Ny Tseng
1709
Primary Peripheral T Cells Become Susceptible to 2,3,7,8-Tetrachlorodibenzo-p-Dioxin-Mediated
Apoptosis in Vitro upon Activation and in the Presence of Dendritic Cell s
Narendra P. Singh, Mitzi Nagarkatti, and Prakash Nagarkatti
1722
Me-Talnetant and Osanetant Interact within Overlapping but Not Identical Binding Pockets in the
Human Tachykinin Neurokinin 3 Receptor Transmembrane Domains
Pari Malherbe, Caterina Bissantz, Anne Marcuz, Claudia Kratzeisen, Marie-Therese Zenner,
Joseph G. Wettstein, Hasane Ratni, Claus Riemer, and Will Spooren
1736
U Novel CYP2C9 Promoter Variants and Assessment of Their Impact on Gene Expression
Melissa A. Kramer, Allan E. Rettie, Mark J. Rieder, Erwin T. Cabacungan, and Ronald N Hines
1751
Identification of the Xenobiotic-Metabolizing Enzyme Arylamine JV-Acetyltransferase 1 as a New
Target of Cisplatin in Breast Cancer Cells: Molecular and Cellular Mechanisms of Inhibition
Nilusha Ragunathan, Julien Dairou, Benjamin Pluvinage, Marta Martins, Emile Petit,
Nathalie Janel, Jean-Marie Dupret, and Fernando Rodrigues-Lima
1761
Covalent Binding of the Nitroso Metabolite of Sulfamethoxazole Is Important in Induction of Drug Specific T-Cell Responses in Vivo
Linling Cheng, Benjamin J. Stewart, Qiang You, Dennis R. Petersen, Joseph A. Ware,
Joseph R. Piccotti, Thomas T. Kawabata, and Cynthia Ju
1769
Potent, Selective and Cell Penetrant Inhibitors of SF-1 by Functional Ultra-High-Throughput
Screening
Franck Madoux, Xiaolin Li, Peter Chase, Gina Zastrow, Michael D. Cameron,
Juliana J. Conkright, Patrick R. Griffin, Scott Thacher, and Peter Hodder
1776
Kavalactones Protect Neural Cells against Amyloid /3 Peptide -Induced Neurotoxicity via Extracellular
Signal-Regulated Kinase 1/2-Dependent Nuclear Factor Erythroid 2-Related Factor 2 Activation
Christoph J. Wruck, Mario E. Gotz, Thomas Herdegen, Deike Varoga, Lars-Ove Brandenburg, and
Thomas Pufe
1785
Partial Deletion of the Nicotinic Cholinergic Receptor a4 or /32 Subunit Genes Changes the
Acetylcholine Sensitivity of Receptor-Mediated 86Rb+ Efflux in Cortex and Thalamus and Alters
Relative Expression of a4 and j32 Subunits
Cecilia Gotti, Milena Moretti, Natalie M. Meinerz, Francesco Clementi, Annalisa Gaimarri,
Allan C. Collins, and Michael J. Marks
1796
Amiloride Derivatives and a Nonpeptidic Antagonist Bind at Two Distinct Allosteric Sites in the
Human Gonadotropin-Releasing Hormone Receptor
Laura H. Heitman, Kai Ye, Julia Oosterom, and Adriaan P. IJzerman
1808
Activation of Tyrosine Hydroxylase mRNA Translation by cAMP in Midbrain Dopaminergic Neurons
Xiqun Chen, Lu Xu, Pheona Radcliffe, Baoyong Sun, and A. William Tank
1816
ATP Modulates Poly(ADP-Ribose) Polymerase-1-Facilitated Topoisomerase I-Linked DNA Religation in the
Presence of Camptothecin
Shin-Young Park, Chung-Hang Leung, and Yung-Chi Cheng
1829
Sazetidine-A Is a Potent and Selective Agonist at Native and Recombinant a4/32 Nicotinic
Acetylcholine Receptors
Ruud Zwart, Anna L. Carbone, Mirko Moroni, Isabel Bermudez, Adrian J. Mogg,
Elizabeth A. Folly, Lisa M. Broad, Andrew C. Williams, Deyi Zhang, Chunjin Ding,
Beverly A. Heinz, and Emanuele Sher
1838
Phenotype of the Cyplal/la2/lbl(-/-) Triple-Knockout Mouse
Nadine Dragin, Zhanquan Shi, Rajat Madan, Christopher L. Karp, Maureen A. Sartor, Chi Chen,
Frank J. Gonzalez, and Daniel W. Nebert
1844
In Vivo Inhibition of Serine Protease Processing Requires a High Fractional Inhibition of Cathepsin C
Nathalie Methot, Daniel Guay, Joel Rubin, Diane Ethier, Karen Ortega, Simon Wong,
Denis Normandin, Christian Beaulieu, T, Jagadeeswar Reddy, Denis Riendeau, and
M. David Percival
1857
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ERRATA
Correction to "a2 Subunit Specificity of Cyclothiazide Inhibition on Glycine Receptors"
1866
Correction to Table of Contents (Volume 73, Number 4, April 2008)
1867