Mol Pharm -- Table of Contents (57 [5])

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May 2000; 57 (5)   [Index by Author] [Cover Caption]

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Minireview:

Erik De Clercq: Inhibition of HIV Infection by Bicyclams, Highly Potent and Specific CXCR4 Antagonists
Mol Pharmacol 2000 57: 833-839. [Abstract] [Full Text] [PDF]

Accelerated Communication:

Rennolds S. Ostrom, Jonathan D. Violin, Scott Coleman, and Paul A. Insel: Selective Enhancement of $beta$ -Adrenergic Receptor Signaling by Overexpression of Adenylyl Cyclase Type 6: Colocalization of Receptor and Adenylyl Cyclase in Caveolae of Cardiac Myocytes
Mol Pharmacol 2000 57: 1075-1079. [Abstract] [Full Text] [PDF]

Articles:

Patricia S. Lorenzo, Maryam Beheshti, George R. Pettit, James C. Stone, and Peter M. Blumberg: The Guanine Nucleotide Exchange Factor RasGRP Is a High -Affinity Target for Diacylglycerol and Phorbol Esters
Mol Pharmacol 2000 57: 840-846. [Abstract] [Full Text] [PDF]

Natalia Filippova, Anna Sedelnikova, Yinong Zong, Henry Fortinberry, and David S. Weiss: Regulation of Recombinant $gamma$ -Aminobutyric Acid (GABA)_A and GABA_C Receptors by Protein Kinase C
Mol Pharmacol 2000 57: 847-856. [Abstract] [Full Text] [PDF]

Judith C. W. Mak, Ad F. Roffel, Toshio Katsunuma, Carolina R. S. Elzinga, Johan Zaagsma, and Peter J. Barnes: Up-Regulation of Airway Smooth Muscle Histamine H₁ Receptor mRNA, Protein, and Function by $beta$ ₂-Adrenoceptor Activation
Mol Pharmacol 2000 57: 857-864. [Abstract] [Full Text] [PDF]

Sheng-Nan Wu, Hui-Fang Li, and Hung-Ting Chiang: Stimulatory Effects of $delta$ -Hexachlorocyclohexane on Ca²⁺-Activated K⁺ Currents in GH₃ Lactotrophs
Mol Pharmacol 2000 57: 865-874. [Abstract] [Full Text] [PDF]

Julie E. Dalziel, Graeme B. Cox, Peter W. Gage, and Bryndis Birnir: Mutating the Highly Conserved Second Membrane-Spanning Region 9' Leucine Residue in the $alpha$ ₁ or $beta$ ₁ Subunit Produces Subunit-Specific Changes in the Function of Human $alpha$ ₁ $beta$ ₁ $gamma$ -Aminobutyric Acid_A Receptors
Mol Pharmacol 2000 57: 875-882. [Abstract] [Full Text] [PDF]

Sang-Hun Lee, Mi-yoon Chang, Ki-Hwan Lee, Byung Sup Park, Young-Seek Lee, Hemin R. Chin, and Yong-Sung Lee: Importance of Valine at Position 152 for the Substrate Transport and 2 $beta$ -Carbomethoxy-3 $beta$ -(4-fluorophenyl)tropane Binding of Dopamine Transporter
Mol Pharmacol 2000 57: 883-889. [Abstract] [Full Text] [PDF]

Astrid E. Alewijnse, Henk Timmerman, Edwin H. Jacobs, Martine J. Smit, Edwin Roovers, Susanna Cotecchia, and Rob Leurs: The Effect of Mutations in the DRY Motif on the Constitutive Activity and Structural Instability of the Histamine H₂ Receptor
Mol Pharmacol 2000 57: 890-898. [Abstract] [Full Text] [PDF]

Takahito Nishiyama, Kenichiro Ogura, Haruhiro Okuda, Kazuma Suda, Atsushi Kato, and Tadashi Watabe: Mechanism-Based Inactivation of Human Dihydropyrimidine Dehydrogenase by (E)-5-(2-Bromovinyl)uracil in the Presence of NADPH
Mol Pharmacol 2000 57: 899-905. [Abstract] [Full Text] [PDF]

Fabrice Duprat, Florian Lesage, Amanda J. Patel, Michel Fink, Georges Romey, and Michel Lazdunski: The Neuroprotective Agent Riluzole Activates the Two P Domain K⁺ Channels TREK-1 and TRAAK
Mol Pharmacol 2000 57: 906-912. [Abstract] [Full Text] [PDF]

Paul Whiteaker, J. Michael McIntosh, Siqin Luo, Allan C. Collins, and Michael J. Marks: ¹²⁵I- $alpha$ -Conotoxin MII Identifies a Novel Nicotinic Acetylcholine Receptor Population in Mouse Brain
Mol Pharmacol 2000 57: 913-925. [Abstract] [Full Text] [PDF]

Charles Kennedy, Ai-Dong Qi, Christopher L. Herold, T. Kendall Harden, and Robert A. Nicholas: ATP, an Agonist at the Rat P2Y₄ Receptor, Is an Antagonist at the Human P2Y₄ Receptor
Mol Pharmacol 2000 57: 926-931. [Abstract] [Full Text] [PDF]

Amy M. Kucken, David A. Wagner, Peter R. Ward, Jeremy A. Teissére, Andrew J. Boileau, and Cynthia Czajkowski: Identification of Benzodiazepine Binding Site Residues in the $gamma$ 2 Subunit of the $gamma$ -Aminobutyric Acid_A Receptor
Mol Pharmacol 2000 57: 932-939. [Abstract] [Full Text] [PDF]

Yuji Ishii, Antony J. Hansen, and Peter I. Mackenzie: Octamer Transcription Factor-1 Enhances Hepatic Nuclear Factor-1 $alpha$ -Mediated Activation of the Human UDP Glucuronosyltransferase 2B7 Promoter
Mol Pharmacol 2000 57: 940-947. [Abstract] [Full Text] [PDF]

Benoit Schneider, Ricardo Biondi, Robert Sarfati, Fabrice Agou, Catherine Guerreiro, Dominique Deville-Bonne, and Michel Veron: The Mechanism of Phosphorylation of Anti-HIV D4T by Nucleoside Diphosphate Kinase
Mol Pharmacol 2000 57: 948-953. [Abstract] [Full Text] [PDF]

Heidi Pelemans, Robert Esnouf, Erik De Clercq, and Jan Balzarini: Mutational Analysis of Trp-229 of Human Immunodeficiency Virus Type 1 Reverse Transcriptase (RT) Identifies This Amino Acid Residue as a Prime Target for the Rational Design of New Non-Nucleoside RT Inhibitors
Mol Pharmacol 2000 57: 954-960. [Abstract] [Full Text] [PDF]

Hongying Zhong, T. J. Murphy, and Kenneth P. Minneman: Activation of Signal Transducers and Activators of Transcription by $alpha$ _1A-Adrenergic Receptor Stimulation in PC12 Cells
Mol Pharmacol 2000 57: 961-967. [Abstract] [Full Text] [PDF]

Katia Varani, Stefania Merighi, Stefania Gessi, Karl-Norbert Klotz, Edward Leung, Pier Giovanni Baraldi, Barbara Cacciari, Romeo Romagnoli, Giampiero Spalluto, and Pier Andrea Borea: [³H]MRE 3008F20: A Novel Antagonist Radioligand for the Pharmacological and Biochemical Characterization of Human A₃ Adenosine Receptors
Mol Pharmacol 2000 57: 968-975. [Abstract] [Full Text] [PDF]

Toshimasa Ishizaki, Masayoshi Uehata, Ichiro Tamechika, Jeongsin Keel, Kimiko Nonomura, Midori Maekawa, and Shuh Narumiya: Pharmacological Properties of Y-27632, a Specific Inhibitor of Rho-Associated Kinases
Mol Pharmacol 2000 57: 976-983. [Abstract] [Full Text] [PDF]

Yan Jin, Farah Sheikh, Karen A. Detillieux, and Peter A. Cattini: Role for Early Growth Response-1 Protein in $alpha$ ₁-Adrenergic Stimulation of Fibroblast Growth Factor-2 Promoter Activity in Cardiac Myocytes
Mol Pharmacol 2000 57: 984-990. [Abstract] [Full Text] [PDF]

Sarah B. Herman, Dawn M. Juilfs, Eric B. Fauman, Paul Juneau, and Joseph P. Menetski: Analysis of a Mutation in Phosphodiesterase Type 4 that Alters Both Inhibitor Activity and Nucleotide Selectivity
Mol Pharmacol 2000 57: 991-999. [Abstract] [Full Text] [PDF]

Paul L. Prather, Nancy A. Martin, Christopher S. Breivogel, and Steven R. Childers: Activation of Cannabinoid Receptors in Rat Brain by WIN 55212-2 Produces Coupling to Multiple G Protein $alpha$ -Subunits with Different Potencies
Mol Pharmacol 2000 57: 1000-1010. [Abstract] [Full Text] [PDF]

Zhigang Yu, Linn M. Huse, Peter Adler, LeRae Graham, Jixiang Ma, Darryl C. Zeldin, and Deanna L. Kroetz: Increased CYP2J Expression and Epoxyeicosatrienoic Acid Formation in Spontaneously Hypertensive Rat Kidney
Mol Pharmacol 2000 57: 1011-1020. [Abstract] [Full Text] [PDF]

Heddwen L. Brooks, John W. Regan, and Andrea J. Yool: Inhibition of Aquaporin-1 Water Permeability by Tetraethylammonium: Involvement of the Loop E Pore Region
Mol Pharmacol 2000 57: 1021-1026. [Abstract] [Full Text] [PDF]

Patricia Casas-González, José Vázquez-Prado, and J. Adolfo García-Sáinz: Lysophosphatidic Acid Modulates $alpha$ _1b-Adrenoceptor Phosphorylation and Function: Roles of Gi and Phosphoinositide 3-Kinase
Mol Pharmacol 2000 57: 1027-1033. [Abstract] [Full Text] [PDF]

Bart J. B. Francken, Katty Josson, Peter Lijnen, Mirek Jurzak, Walter H. M. L. Luyten, and Josée E. Leysen: Human 5-Hydroxytryptamine_5A Receptors Activate Coexpressed G_i and G_o Proteins in Spodoptera frugiperda 9 Cells
Mol Pharmacol 2000 57: 1034-1044. [Abstract] [Full Text] [PDF]

Waldemar Gonsiorek, Charles Lunn, Xuedong Fan, Satwant Narula, Daniel Lundell, and R. William Hipkin: Endocannabinoid 2-Arachidonyl Glycerol Is a Full Agonist through Human Type 2 Cannabinoid Receptor: Antagonism by Anandamide
Mol Pharmacol 2000 57: 1045-1050. [Abstract] [Full Text] [PDF]

Helene Pelicano, Marina Kukhanova, and Yung-Chi Cheng: Excision of $beta$ -D- and $beta$ -L-Nucleotide Analogs from DNA by the Human Cytosolic 3'-to-5' Exonuclease
Mol Pharmacol 2000 57: 1051-1055. [Abstract] [Full Text] [PDF]

Guillermo Elizondo, Pedro Fernandez-Salguero, M. Saeed Sheikh, Geum-Yi Kim, Albert J. Fornace, Kyung S. Lee, and Frank J. Gonzalez: Altered Cell Cycle Control at the G₂/M Phases in Aryl Hydrocarbon Receptor-Null Embryo Fibroblast
Mol Pharmacol 2000 57: 1056-1063. [Abstract] [Full Text] [PDF]

Arthur A. Simen and Richard J. Miller: Involvement of Regions in Domain I in the Opioid Receptor Sensitivity of $alpha$ 1B Ca²⁺ Channels
Mol Pharmacol 2000 57: 1064-1074. [Abstract] [Full Text] [PDF]

Cover Caption:

About the cover: Model for the activation of oxytocin receptors. The left panel shows a minimized structure of a constitutivelyactive mutant of the human oxytocin receptor. The right panelshows a model of the interaction between oxytocin and the wild-typereceptor, and for comparison the center panel shows a complexbetween oxytocin and inactive mutant of the receptor. Receptorsare depicted as helix ribbon bundles in cross-section throughthe surface membrane, with the intracellular surface at the topand the extracellular surface at the bottom. The solvent-accessiblesurfaces are represented by dot-clouds and predict that the activationprocess involves the opening of a solvent-exposed cytosolic crevice.From Fanelli F, Barbier P, Zanchetta D, de Benedetti PG and ChiniB (1999) Activation mechanism of human oxytocin receptor: A combinedstudy of experimental and computer-simulated mutagenesis. MolPharmacol 56:214-225.