Mol Pharm -- Table of Contents (62 [1])

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July 2002; 62 (1)   [Index by Author] [Cover Caption]

       Accelerated Communications

       Articles

       Errata

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Accelerated Communications:

Chava Kimchi-Sarfaty, John J. Gribar, and Michael M. Gottesman: Functional Characterization of Coding Polymorphisms in the Human MDR1 Gene Using a Vaccinia Virus Expression System
Mol Pharmacol 2002 62: 1-6. [Abstract] [Full Text] [PDF]

Articles:

Yasuna Kobayashi, Naomi Ohshiro, Akiko Shibusawa, Tadanori Sasaki, Shogo Tokuyama, Takashi Sekine, Hitoshi Endou, and Toshinori Yamamoto: Isolation, Characterization and Differential Gene Expression of Multispecific Organic Anion Transporter 2 in Mice
Mol Pharmacol 2002 62: 7-14. [Abstract] [Full Text] [PDF]

María L. López-Rodríguez, Bruno Vicente, Xavier Deupi, Sergio Barrondo, Mireia Olivella, M. José Morcillo, Bellinda Behamú, Juan A. Ballesteros, Joan Sallés, and Leonardo Pardo: Design, Synthesis and Pharmacological Evaluation of 5-Hydroxytryptamine_1a Receptor Ligands to Explore the Three-Dimensional Structure of the Receptor
Mol Pharmacol 2002 62: 15-21. [Abstract] [Full Text] [PDF]

Peter C. Waldmeier, Jean-Jacques Feldtrauer, Ting Qian, and John J. Lemasters: Inhibition of the Mitochondrial Permeability Transition by the Nonimmunosuppressive Cyclosporin Derivative NIM811
Mol Pharmacol 2002 62: 22-29. [Abstract] [Full Text] [PDF]

Lene Martini, Hanne Hastrup, Birgitte Holst, Alberto Fraile-Ramos, Mark Marsh, and Thue W. Schwartz: NK1 Receptor Fused to $beta$ -Arrestin Displays a Single-Component, High-Affinity Molecular Phenotype
Mol Pharmacol 2002 62: 30-37. [Abstract] [Full Text] [PDF]

Niu Shin, Elizabeth Coates, Nicholas J. Murgolo, Kelley L. Morse, Marvin Bayne, Catherine D. Strader, and Frederick J. Monsma, Jr.: Molecular Modeling and Site-Specific Mutagenesis of the Histamine-Binding Site of the Histamine H₄ Receptor
Mol Pharmacol 2002 62: 38-47. [Abstract] [Full Text] [PDF]

Pierre Escoubas, Sylvie Diochot, Marie-Louise Célérier, Terumi Nakajima, and Michel Lazdunski: Novel Tarantula Toxins for Subtypes of Voltage-Dependent Potassium Channels in the Kv2 and Kv4 Subfamilies
Mol Pharmacol 2002 62: 48-57. [Abstract] [Full Text] [PDF]

N. J. Laping, E. Grygielko, A. Mathur, S. Butter, J. Bomberger, C. Tweed, W. Martin, J. Fornwald, R. Lehr, J. Harling, L. Gaster, J. F. Callahan, and B. A. Olson: Inhibition of Transforming Growth Factor (TGF)- $beta$ 1-Induced Extracellular Matrix with a Novel Inhibitor of the TGF- $beta$ Type I Receptor Kinase Activity: SB-431542
Mol Pharmacol 2002 62: 58-64. [Abstract] [Full Text] [PDF]

Gareth J. Inman, Francisco J. Nicolás, James F. Callahan, John D. Harling, Laramie M. Gaster, Alastair D. Reith, Nicholas J. Laping, and Caroline S. Hill: SB-431542 Is a Potent and Specific Inhibitor of Transforming Growth Factor- $beta$ Superfamily Type I Activin Receptor-Like Kinase (ALK) Receptors ALK4, ALK5, and ALK7
Mol Pharmacol 2002 62: 65-74. [Abstract] [Full Text] [PDF]

Yoshifumi Kawanabe, Yasuo Okamoto, Soichi Miwa, Nobuo Hashimoto, and Tomoh Masaki: Molecular Mechanisms for the Activation of Voltage-Independent Ca²⁺ Channels by Endothelin-1 in Chinese Hamster Ovary Cells Stably Expressing Human Endothelin_A Receptors
Mol Pharmacol 2002 62: 75-80. [Abstract] [Full Text] [PDF]

Zhan-Guo Gao, Seong Gon Kim, Kelly A. Soltysiak, Neli Melman, Adriaan P. IJzerman, and Kenneth A. Jacobson: Selective Allosteric Enhancement of Agonist Binding and Function at Human A₃ Adenosine Receptors by a Series of Imidazoquinoline Derivatives
Mol Pharmacol 2002 62: 81-89. [Abstract] [Full Text] [PDF]

Chin-Ju Tsi, Yee Chao, Ching-Wen Chen, and Wan Wan Lin: Aurintricarboxylic Acid Protects against Cell Death Caused by Lipopolysaccharide in Macrophages by Decreasing Inducible Nitric-Oxide Synthase Induction via I $kappa$ B Kinase, Extracellular Signal-Regulated Kinase, and p38 Mitogen-Activated Protein Kinase Inhibition
Mol Pharmacol 2002 62: 90-101. [Abstract] [Full Text] [PDF]

Sally A. Coulthard, Linda A. Hogarth, Margaret Little, Elizabeth C. Matheson, Christopher P. F. Redfern, Lynne Minto, and Andrew G. Hall: The Effect of Thiopurine Methyltransferase Expression on Sensitivity to Thiopurine Drugs
Mol Pharmacol 2002 62: 102-109. [Abstract] [Full Text] [PDF]

Jennifer L. Vuletich, Ezra R. Lowe, Suree Jianmongkol, Yasuhiko Kamada, Ute M. Kent, Andrew T. Bender, Damon R. Demady, Paul F. Hollenberg, and Yoichi Osawa: Alteration of the Heme Prosthetic Group of Neuronal Nitric-Oxide Synthase during Inactivation by N^G-Amino-L-arginine in Vitro and in Vivo
Mol Pharmacol 2002 62: 110-118. [Abstract] [Full Text] [PDF]

Eldo V. Kuzhikandathil and Gerry S. Oxford: Classic D1 Dopamine Receptor Antagonist R-(+)-7-Chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (SCH23390) Directly Inhibits G Protein-Coupled Inwardly Rectifying Potassium Channels
Mol Pharmacol 2002 62: 119-126. [Abstract] [Full Text] [PDF]

Benzy J. Padanilam, Tong Lu, Toshinori Hoshi, Beena A. Padanilam, Erwin F. Shibata, and Hon-Chi Lee: Molecular Determinants of Intracellular pH Modulation of Human Kv1.4 N-Type Inactivation
Mol Pharmacol 2002 62: 127-134. [Abstract] [Full Text] [PDF]

Thomas K. Knott, Alejandro M. Dopico, Govindan Dayanithi, José Lemos, and Steven N. Treistman: Integrated Channel Plasticity Contributes to Alcohol Tolerance in Neurohypophysial Terminals
Mol Pharmacol 2002 62: 135-142. [Abstract] [Full Text] [PDF]

Mary J. Kuffel, Jennifer C. Schroeder, Lori J. Pobst, Stephen Naylor, Joel M. Reid, Scott H. Kaufmann, and Matthew M. Ames: Activation of the Antitumor Agent Aminoflavone (NSC 686288) Is Mediated by Induction of Tumor Cell Cytochrome P450 1A1/1A2
Mol Pharmacol 2002 62: 143-153. [Abstract] [Full Text] [PDF]

Philip A. Gregory and Peter I. Mackenzie: The Homeodomain Pbx2-Prep1 Complex Modulates Hepatocyte Nuclear Factor 1 $alpha$ -Mediated Activation of the UDP-Glucuronosyltransferase 2B17 Gene
Mol Pharmacol 2002 62: 154-161. [Abstract] [Full Text] [PDF]

Yvonne S. Lin, Amy L. S. Dowling, Sean D. Quigley, Federico M. Farin, Jiong Zhang, Jatinder Lamba, Erin G. Schuetz, and Kenneth E. Thummel: Co-Regulation of CYP3A4 and CYP3A5 and Contribution to Hepatic and Intestinal Midazolam Metabolism
Mol Pharmacol 2002 62: 162-172. [Abstract] [Full Text] [PDF]

Mieke Gouwy, Sofie Struyf, Frank Mahieu, Willy Put, Paul Proost, and Jo Van Damme: The Unique Property of the CC Chemokine Regakine-1 to Synergize with Other Plasma-Derived Inflammatory Mediators in Neutrophil Chemotaxis Does Not Reside in Its NH₂-Terminal Structure
Mol Pharmacol 2002 62: 173-180. [Abstract] [Full Text] [PDF]

Hugues Greney, Dragan Urosevic, Stephan Schann, Laurence Dupuy, Véronique Bruban, Jean-Daniel Ehrhardt, Pascal Bousquet, and Monique Dontenwill: [¹²⁵I]2-(2-Chloro-4-iodo-phenylamino)-5-methyl-pyrroline (LNP 911), a High-Affinity Radioligand Selective for I₁ Imidazoline Receptors
Mol Pharmacol 2002 62: 181-191. [Abstract] [Full Text] [PDF]

Errata:

: Correction to "Human Bronchial Epithelial and Endothelial Cells Express $alpha$ 7 Nicotinic Acetylcholine Receptors"
Mol Pharmacol 2002 62: 192. [Full Text] [PDF]

Cover Caption:

About the cover: DAT TM3 electrostatic potential models. A, dot surface displays of electrostatic potentials in WT (left)and F154A (right) TM3 helices. Each TM3 was built as an $alpha$ -helixand energy-minimized. The 21 amino acids of TM3 cross the plasmamembrane from the lower (N-terminal, cytoplasmic) side to theupper (C-terminal, extracellular) side. F154A is indicated byarrows. Dot surfaces were displayed using Sybyl 6.6 "vdW Dot Surface"with red indicating electrostatic potential measures of "V" >24.9; orange, yellow or green 3.3 > V > 0, cyan 0 > V > $-$ 3.3 andblue, purple or white V < $-$ 24.9. "V" is defined as described previously[Weiner PA, Langridge R, Blaney JM, Scharfer R, and Kollman PK(1982) Electrostatic potential molecular surfaces. Proc Natl AcadSci USA 79:3754-3758] at an arbitrary distance of 1.4 Å.At the helical side important for cocaine binding, there are sevenresidues; three (42%) are decreased and another three increasedin electrostatic potentials. At the side for dopamine uptake,there are eight residues; seven of them (87%) are decreased andnone of them is increased in electrostatic potentials. Indicatedare amino acid residues visible on this graph to the reader andwhose electrostatic potentials are reduced by the F154A substitution.Italic lables denote residues hiding from the reader (locatedat the opposite side of the domain). #, increased electrostaticpotentials for asparagine 157 (above the arrow) and phenylalanine150 (below the arrow). Scale bar, 5 Å. Mol Pharmacol 61:885-981.