Mol Pharm -- Table of Contents (62 [3])

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September 2002; 62 (3)   [Index by Author] [Cover Caption]

       Perspective

       Accelerated Communications

       Articles

       Errata

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Perspective:

Robert H. Tukey, Christian P. Strassburg, and Peter I. Mackenzie: Pharmacogenomics of Human UDP-Glucuronosyltransferases and Irinotecan Toxicity
Mol Pharmacol 2002 62: 446-450. [Full Text] [PDF]

David R. Manning: Measures of Efficacy Using G Proteins as Endpoints: Differential Engagement of G Proteins through Single Receptors
Mol Pharmacol 2002 62: 451-452. [Full Text] [PDF]

Accelerated Communications:

Thomas Weiser and Nicola Wilson: Inhibition of Tetrodotoxin (TTX)-Resistant and TTX-Sensitive Neuronal Na⁺ Channels by the Secretolytic Ambroxol
Mol Pharmacol 2002 62: 433-438. [Abstract] [Full Text] [PDF]

Erin Schuetz, Lubin Lan, Kazuto Yasuda, Richard Kim, Thomas A. Kocarek, John Schuetz, and Stephen Strom: Development of A Real-Time in Vivo Transcription Assay: Application Reveals Pregnane X Receptor-Mediated Induction of CYP3A4 by Cancer Chemotherapeutic Agents
Mol Pharmacol 2002 62: 439-445. [Abstract] [Full Text] [PDF]

Articles:

G. Weigel, P. Bertalanffy, and E. Wolner: Depletion of Intracellular GTP Results in Nuclear Factor- $kappa$ B Activation and Intercellular Adhesion Molecule-1 Expression in Human Endothelial Cells
Mol Pharmacol 2002 62: 453-462. [Abstract] [Full Text] [PDF]

Min Huang, Yanhong Wang, Matthew Collins, Beverly S. Mitchell, and Lee M. Graves: A77 1726 Induces Differentiation of Human Myeloid Leukemia K562 Cells by Depletion of Intracellular CTP Pools
Mol Pharmacol 2002 62: 463-472. [Abstract] [Full Text] [PDF]

Limin Mao and John Q. Wang: Glutamate Cascade to cAMP Response Element-Binding Protein Phosphorylation in Cultured Striatal Neurons through Calcium-Coupled Group I Metabotropic Glutamate Receptors
Mol Pharmacol 2002 62: 473-484. [Abstract] [Full Text] [PDF]

Ning Qin, Susan Yagel, Mary-Lou Momplaisir, Ellen E. Codd, and Michael R. D'Andrea: Molecular Cloning and Characterization of the Human Voltage-Gated Calcium Channel $alpha$ ₂ $delta$ -4 Subunit
Mol Pharmacol 2002 62: 485-496. [Abstract] [Full Text] [PDF]

Douglas G. Tilley and Donald H. Maurice: Vascular Smooth Muscle Cell Phosphodiesterase (PDE) 3 and PDE4 Activities and Levels are Regulated by Cyclic AMP in Vivo
Mol Pharmacol 2002 62: 497-506. [Abstract] [Full Text] [PDF]

Alicia V. Binda, Nadine Kabbani, Ridwan Lin, and Robert Levenson: D2 and D3 Dopamine Receptor Cell Surface Localization Mediated by Interaction with Protein 4.1N
Mol Pharmacol 2002 62: 507-513. [Abstract] [Full Text] [PDF]

W. Zhang, H. Ke, and R. W. Colman: Identification of Interaction Sites of Cyclic Nucleotide Phosphodiesterase Type 3A with Milrinone and Cilostazol Using Molecular Modeling and Site-Directed Mutagenesis
Mol Pharmacol 2002 62: 514-520. [Abstract] [Full Text] [PDF]

Claudia Alvarado-Castillo, Patricia Lozano-Zarain, Jesús Mateo, T. Kendall Harden, and José L. Boyer: A Fusion Protein of the Human P2Y₁ Receptor and NTPDase1 Exhibits Functional Activities of the Native Receptor and Ectoenzyme and Reduced Signaling Responses to Endogenously Released Nucleotides
Mol Pharmacol 2002 62: 521-528. [Abstract] [Full Text] [PDF]

Yi-He Ling, Jian-Dong Jiang, James F. Holland, and Roman Perez-Soler: Arsenic Trioxide Produces Polymerization of Microtubules and Mitotic Arrest before Apoptosis in Human Tumor Cell Lines
Mol Pharmacol 2002 62: 529-538. [Abstract] [Full Text] [PDF]

Akira Ando, Amy Yang, Hiroyuki Nambu, and Peter A. Campochiaro: Blockade of Nitric-Oxide Synthase Reduces Choroidal Neovascularization
Mol Pharmacol 2002 62: 539-544. [Abstract] [Full Text] [PDF]

Thipparat Suwanmanee, Halina Sierakowska, Giuseppina Lacerra, Saovaros Svasti, Suzanne Kirby, Christopher E. Walsh, Suthat Fucharoen, and Ryszard Kole: Restoration of Human $beta$ -Globin Gene Expression in Murine and Human IVS2-654 Thalassemic Erythroid Cells by Free Uptake of Antisense Oligonucleotides
Mol Pharmacol 2002 62: 545-553. [Abstract] [Full Text] [PDF]

Andriy E. Belevych, Sunita Warrier, and Robert D. Harvey: Genistein Inhibits Cardiac L-Type Ca²⁺ Channel Activity by a Tyrosine Kinase-Independent Mechanism
Mol Pharmacol 2002 62: 554-565. [Abstract] [Full Text] [PDF]

Amy C. Arai, Yan-Fang Xia, Markus Kessler, Dean Phillips, Richard Chamberlin, Richard Granger, and Gary Lynch: Effects of 5'-Alkyl-Benzothiadiazides on (R,S)- $alpha$ -Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Biophysics and Synaptic Responses
Mol Pharmacol 2002 62: 566-577. [Abstract] [Full Text] [PDF]

Didier Cussac, Adrian Newman-Tancredi, Delphine Duqueyroix, Valérie Pasteau, and Mark J. Millan: Differential Activation of Gq/11 and Gi₃ Proteins at 5-Hydroxytryptamine_2C Receptors Revealed by Antibody Capture Assays: Influence of Receptor Reserve and Relationship to Agonist-Directed Trafficking
Mol Pharmacol 2002 62: 578-589. [Abstract] [Full Text] [PDF]

Adrian Newman-Tancredi, Didier Cussac, Laetitia Marini, and Mark J. Millan: Antibody Capture Assay Reveals Bell-Shaped Concentration-Response Isotherms for h5-HT_1A Receptor-Mediated G $alpha$ _i3 Activation: Conformational Selection by High-Efficacy Agonists, and Relationship to Trafficking of Receptor Signaling
Mol Pharmacol 2002 62: 590-601. [Abstract] [Full Text] [PDF]

Libing Li, Isao Matsuoka, Yuichi Suzuki, Yasuhide Watanabe, Toshiyuki Ishibashi, Keiko Yokoyama, Yukio Maruyama, and Junko Kimura: Inhibitory Effect of Fluvastatin on Lysophosphatidylcholine-Induced Nonselective Cation Current in Guinea Pig Ventricular Myocytes
Mol Pharmacol 2002 62: 602-607. [Abstract] [Full Text] [PDF]

Jean-François Gagné, Valerie Montminy, Patrick Belanger, Kim Journault, Genevieve Gaucher, and Chantal Guillemette: Common Human UGT1A Polymorphisms and the Altered Metabolism of Irinotecan Active Metabolite 7-Ethyl-10-hydroxycamptothecin (SN-38)
Mol Pharmacol 2002 62: 608-617. [Abstract] [Full Text] [PDF]

Kirk E. Dineley, Latha M. Malaiyandi, and Ian J. Reynolds: A Reevaluation of Neuronal Zinc Measurements: Artifacts Associated with High Intracellular Dye Concentration
Mol Pharmacol 2002 62: 618-627. [Abstract] [Full Text] [PDF]

Dean J. Naisbitt, John Farrell, S. Fraser Gordon, James L. Maggs, Christoph Burkhart, Werner J. Pichler, Munir Pirmohamed, and B. Kevin Park: Covalent Binding of the Nitroso Metabolite of Sulfamethoxazole Leads to Toxicity and Major Histocompatibility Complex-Restricted Antigen Presentation
Mol Pharmacol 2002 62: 628-637. [Abstract] [Full Text] [PDF]

Jodi M. Maglich, Catherine M. Stoltz, Bryan Goodwin, Diane Hawkins-Brown, John T. Moore, and Steven A. Kliewer: Nuclear Pregnane X Receptor and Constitutive Androstane Receptor Regulate Overlapping but Distinct Sets of Genes Involved in Xenobiotic Detoxification
Mol Pharmacol 2002 62: 638-646. [Abstract] [Full Text] [PDF]

Mustapha Najimi, Jean-Jacques Robert, Jacques Mallet, William Rostène, and Patricia Forgez: Neurotensin Induces Tyrosine Hydroxylase Gene Activation through Nitric Oxide and Protein Kinase C Signaling Pathways
Mol Pharmacol 2002 62: 647-653. [Abstract] [Full Text] [PDF]

Wendy Cladman and Peter Chidiac: Characterization and Comparison of RGS2 and RGS4 as GTPase-Activating Proteins for m2 Muscarinic Receptor-Stimulated G_i
Mol Pharmacol 2002 62: 654-659. [Abstract] [Full Text] [PDF]

Linnea M. Baudhuin, Kelly L. Cristina, Jun Lu, and Yan Xu: Akt Activation Induced by Lysophosphatidic Acid and Sphingosine-1-phosphate Requires Both Mitogen-Activated Protein Kinase Kinase and p38 Mitogen-Activated Protein Kinase and Is Cell-Line Specific
Mol Pharmacol 2002 62: 660-671. [Abstract] [Full Text] [PDF]

Fatih Özdener, Carol Dangelmaier, Barrie Ashby, Satya P. Kunapuli, and James L. Daniel: Activation of Phospholipase C $gamma$ 2 by Tyrosine Phosphorylation
Mol Pharmacol 2002 62: 672-679. [Abstract] [Full Text] [PDF]

Deepa Sampath, Zheng Shi, and William Plunkett: Inhibition of Cyclin-Dependent Kinase 2 by the Chk1-Cdc25A Pathway during the S-Phase Checkpoint Activated by Fludarabine: Dysregulation by 7-Hydroxystaurosporine
Mol Pharmacol 2002 62: 680-688. [Abstract] [Full Text] [PDF]

Valerie Levresse, Lindsay Marek, Deborah Blumberg, and Lynn E. Heasley: Regulation of Platinum-Compound Cytotoxicity by the c-Jun N-Terminal Kinase and c-Jun Signaling Pathway in Small-Cell Lung Cancer Cells
Mol Pharmacol 2002 62: 689-697. [Abstract] [Full Text] [PDF]

Riku Korhonen, Aleksi Lahti, Mari Hämäläinen, Hannu Kankaanranta, and Eeva Moilanen: Dexamethasone Inhibits Inducible Nitric-Oxide Synthase Expression and Nitric Oxide Production by Destabilizing mRNA in Lipopolysaccharide-Treated Macrophages
Mol Pharmacol 2002 62: 698-704. [Abstract] [Full Text] [PDF]

David A. Andersson, Mikael Adner, Edward D. Högestätt, and Peter M. Zygmunt: Mechanisms Underlying Tissue Selectivity of Anandamide and Other Vanilloid Receptor Agonists
Mol Pharmacol 2002 62: 705-713. [Abstract] [Full Text] [PDF]

Leen De Bolle, Detlef Michel, Thomas Mertens, Chaysavanh Manichanh, Henri Agut, Erik De Clercq, and Lieve Naesens: Role of the Human Herpesvirus 6 U69-Encoded Kinase in the Phosphorylation of Ganciclovir
Mol Pharmacol 2002 62: 714-721. [Abstract] [Full Text] [PDF]

Carl E. Ruby, Mark Leid, and Nancy I. Kerkvliet: 2,3,7,8-Tetrachlorodibenzo-p-dioxin Suppresses Tumor Necrosis Factor- $alpha$ and Anti-CD40-Induced Activation of NF- $kappa$ B/Rel in Dendritic Cells: p50 Homodimer Activation Is Not Affected
Mol Pharmacol 2002 62: 722-728. [Abstract] [Full Text] [PDF]

Sannah Zoffmann, André Chollet, and Jean-Luc Galzi: Identification of the Extracellular Loop 2 as the Point of Interaction between the N Terminus of the Chemokine MIP-1 $alpha$ and Its CCR1 Receptor
Mol Pharmacol 2002 62: 729-736. [Abstract] [Full Text] [PDF]

Stephen S. Ferguson, Edward L. LeCluyse, Masahiko Negishi, and Joyce A. Goldstein: Regulation of Human CYP2C9 by the Constitutive Androstane Receptor: Discovery of a New Distal Binding Site
Mol Pharmacol 2002 62: 737-746. [Abstract] [Full Text] [PDF]

Alison J. McLean, Fu-Yue Zeng, Dominic Behan, Derek Chalmers, and Graeme Milligan: Generation and Analysis of Constitutively Active and Physically Destabilized Mutants of the Human $beta$ ₁-Adrenoceptor
Mol Pharmacol 2002 62: 747-755. [Abstract] [Full Text] [PDF]

Yoshifumi Kawanabe, Nobuo Hashimoto, and Tomoh Masaki: Effects of Phosphoinositide 3-Kinase on the Endothelin-1-Induced Activation of Voltage-Independent Ca²⁺ Channels and Mitogenesis in Chinese Hamster Ovary Cells Stably Expressing Endothelin_A Receptor
Mol Pharmacol 2002 62: 756-761. [Abstract] [Full Text] [PDF]

Errata:

: Correction to "Negative and positive regulatory epitopes in the C-terminal domains of the human B1 and B2 bradykinin receptor subtypes determine receptor coupling efficacy to G_9/11-mediated phospholipase C $beta$ activity "
Mol Pharmacol 2002 62: 762. [Full Text] [PDF]

: Correction to "Behavioral characterization of mice lacking histamine H₃ receptors"
Mol Pharmacol 2002 62: 763. [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.