Designing Transcription Factor Architectures for Drug Discovery

MOLECULAR

______PHARMACOLOGY December 2004 Volume 66 Number 6 http://molpharm.aspetjournals.org ISSN 0026-895X

MINIREVIEW Designing Transcription Factor Architectures for Drug Discovery Pilar Blancafort, David J. Segal, and Carlos F. Barbas III 1 361

ARTICLES Oxidative Stress and Mitochondrial Aldehyde Dehydrogenase Activity: A Comparison of Pentaerythritol Tetranitrate with Other Organic Nitrates Andreas Daiber, Matthias Oelze, Meike Coldewey, Markus Bachschmid, Philip Wenzel, Karsten Sydow, Maria Wendt, Andrei L. Kleschyov, Dirk Stalleicken, Volker Ullrich, Alexander Miilsch, and Thomas Mu'nzel 1372

Critical Role of Reactive Oxygen Species and Mitochondrial Membrane Potential in Korean Mistletoe Lectin-Induced Apoptosis in Human Hepatocarcinoma Cells Won-Ho Kim, Won Bong Park, Bin Gao, and Myeong Ho Jung 1383

Analysis of ATP-Binding Cassette Transporter Expression in Drug-Selected Cell Lines by a Microarray Dedicated to Multidrug Resistance Jean-Philippe Annereau, Gergely Szakdcs, Charles J. Tucker, Angela Arciello, Carol Cardarelli, Jennifer Collins, Sherry Grissom, Barry R. Zeeberg, William Reinhold, John N. Weinstein, Yves Pommier, Richard S. Paules, and Michael M. Gottesman 1397

Ligand Binding and Kinetics of Folate Receptor Recycling in Vivo: Impact on Receptor-Mediated Drug Delivery Chrystal M. Paulos, Joseph A. Reddy, Christopher P. Leamon, Mary Jo Turk, and Philip S. Low 1406

Doxorubicin Inhibits DNMT1, Resulting in Conditional Apoptosis Tomoki Yokochi and Keith D. Robertson 1415

Low-Affinity Neurotensin Receptor (NTS2) Signaling: Internalization-Dependent Activation of Extracellular Signal-Regulated Kinases 1/2 Louis Gendron, Amelie Perron, Marcel Daniel Payet, Nicole Gallo-Payet, Philippe Sarret, and Alain Beaudet 1421 Viral Macrophage Inflammatory Protein-II and Fractalkine (CX3CL1) Chimeras Identify Molecular Determinants of Affinity, Efficacy, and Selectivity at CX3CR1 Christopher N. Davis, Violetta Zujovic, and Jeffrey K. Harrison 1431

Overlapping Transcriptional Programs Regulated by the Nuclear Receptors Peroxisome Proliferator- Activated Receptor a, Retinoid X Receptor, and Liver X Receptor in Mouse Liver Steven P. Anderson, Corrie Dunn, Ashley Laughter, Lawrence Yoon, Cynthia Swanson, Thomas M. Stulnig, Knut R. Steffensen, Roshantha A.S. Chandraratna, Jan-Ake Gustafsson, and J. Christopher Gorton

Single-Cell Imaging of Intracellular Ca2+ and Phospholipase C Activity Reveals That RGS 2, 3, and 4 Differentially Regulate Signaling via the Gaq/11-Linked Muscarinic M3 Receptor Stephen C. Tovey and Gary B. Willars 1453

Induction of Cyclooxygenase-2 Overexpression in Human Gastric Epithelial Cells by Helicobacter pylori Involves TLR2/TLR9 and c-Src-Dependent Nuclear Factor-«B Activation Ya Jen Chang, Ming Shiang Wu, Jaw Town Lin, Bor Shyang Sheu, Tatsushi Muta, Hiroyasu Inoue, and Ching-Chow Chen 1465

Evidence That Mitogen-Activated Protein Kinase Phosphatase-1 Induction by Proteasome Inhibitors Plays an Antiapoptotic Role George W. Small, Yue Y. Shi, Natalie A. Edmund, Sivagurunathan Somasundaram, Dominic T. Moore, and Robert Z. Orlowski 1478

Certain 1,4-Disubstituted Aromatic Piperidines and Piperazines with Extreme Selectivity for the Dopamine D4 Receptor Interact with a Common Receptor Microdomain Sandhya Kortagere, Peter Gmeiner, Harel Weinstein, and John A. Schetz 1491

Regulation of Cyclin-Dependent Kinase 5 and Calcium/Calmodulin-Dependent Protein Kinase II by Phosphatidylinositol-Linked Dopamine Receptor in Rat Brain Xuechu Zhen, Satindra Goswami, Syed Amir Abdali, Mara Gil, Kalindi Bakshi, and Eitan Friedman 1500

Gaz Inhibits Serum Response Factor-Dependent Transcription by Inhibiting Rho Signaling Parmesh Dutt, Aron B. Jaffe, Keith D. Merdek, Alan Hall, and Deniz Toksoz 1508

Multiple Actions of Propofol on afiy and a/3S GABAA Receptors Hua-Jun Feng and Robert L. Macdonald 1517

Selective Modulation of Ligand-Gated P2X Purinoceptor Channels by Acute Hypoxia Is Mediated by Reactive Oxygen Species H. S. Mason, S. Bourke, and P. J. Kemp 1525

Impaired CREB-1 Phosphorylation in Antifolate-Resistant Cell Lines with Down-Regulation of the Reduced Folate Carrier Gene Lilah Rothem, Michal Stark, and Yehuda G. Assaraf 1536

Signaling and Ligand Binding by Recombinant Neuromedin U Receptors: Evidence for Dual Coupling to Gaq/11 and Gc^ and an Irreversible Ligand-Receptor Interaction Paul J. Brighton, Philip G. Szekeres, Alan Wise, and Gary B. Willars 1544

A Novel Computational Approach for the Prediction of Networked Transcription Factors of Aryl Hydrocarbon-Receptor-Regulated Genes Alexander Kel, Susanne Reymann, Volker Matys, Paul Nettesheim, Edgar Wingender, and Jiirgen Borlak 1557

Mechanisms of Agonist Action at D2 Dopamine Receptors David J. Roberts, Hong Lin, and Philip G. Strange 1573

Differential Expression of /x-Opioid Receptor Gene in CXBK and B6 Mice by Spl Po-Wei Lee, Sally Wu, and Yu-May Lee 1580 Protocols for Regulation and Study of Diphosphoinositol Polyphosphates S. T. Safrany 1585 Protein Kinase C Activation Enhances Morphine-Induced Rapid Desensitization of /i-Opioid Receptors in Mature Rat Locus Ceruleus Neurons Christopher P. Bailey, Eamonn Kelly, and Graeme Henderson

1592 Suppression of Pathogenicity of Porphyromonas gingivalis by Newly Developed Gingipain Inhibitors Tomoko Kadowaki, Atsuyo Baba, Naoko Abe, Ryosuke Takii, Munetaka Hashimoto, Takayuki Tsukuba, Shinji Okazaki, Yoshimitsu Suda, Tetsuji Asao, and Kenji Yamamoto 1599 Enhancement of Cardiac L-Type Ca2+ Currents in Transgenic Mice with Cardiac-Specific Overexpression of CYP2J2 Yong-Fu Xiao, Qingen Ke, John M. Seubert, J. Alyce Bradbury, Joan Graves, Laura M. DeGraff, John R. Falck, Kris Krausz,_ Harry V. Gelboin, James P. Morgan, and Darryl C. Zeldin 1607

Using Molecular Tools to Dissect the Role of Gas in Sensitization of AC1 Timothy A. Vortherms, Chau H. Nguyen, Catherine H. Berlot, and Val J. Watts 1617 Alterations in Receptor Expression or Agonist Concentration Change the Pathways Gastrin-Releasing Peptide Receptor Uses to Regulate Extracellular Signal-Regulated Kinase Pei-Wen Chen and Glenn S. Kroog 1625 Preferential Interaction between the Dopamine D2 Receptor and Arrestin2 in Neostriatal Neurons Tara A. Macey, Vsevolod V. Gurevich, and Kim A, Neve 1635 Up-Regulation of Cyclooxygenase-2 Expression Is Involved in it!( + )-Methanandamide-Induced Apoptotic Death of Human Neuroglioma Cells Burkhard Him, Robert Ramer, Karin Eichele, Ulrike Weinzierl, and Kay Brune 1643

State-Dependent Mibefradil Block of Na+ Channels Megan M. McNulty and Dorothy A. Hanck 1652 2,3,7,8-Tetrachlorodibenzo-p-dioxin Induces Suppressor of Cytokine Signaling 2 in Murine B Cells Darrell R. Boverhof, Elaine Tarn, Allison S. Harney, Robert B. Crawford, Norbert E. Kaminski, and Timothy R. Zacharewski 1662 Specificity of the Dihydroceramide Desaturase Inhibitor A^-[(lfi,2S)-2-Hydroxy-l-hydroxymethyl-2-(2- tridecyl-l-cyclopropenyl)ethyl]octanamide (GT11) in Primary Cultured Cerebellar Neurons Gemma Triola, Gemma Fabrias, Mihaela Dragusin, Lars Niederhausen, Roland Broere, Amadeu Llebaria, and Gerhild van Echten-Deckert 1671 Discovery of BRL 50481 [3-(A^-dimethylsulfonamido)-4-methyl-nitrobenzene], a Selective Inhibitor of Phosphodiesterase 7: In Vitro Studies in Human Monocytes, Lung Macrophages, and CD8 + T- Lymphocytes Susan J. Smith, Lenora B. Cieslinski, Robert Newton, Louise E. Donnelly, Peter S. Fenwick, Andrew G. Nicholson, Peter J. Barnes, Mary S. Barnette, and Mark A. Giembycz 1679 The Human Sulfotransferase SULT1A1 Gene Is Regulated in a Synergistic Manner by Spl and GA Binding Protein Nadine Hempel, Hongbing Wang, Edward L. LeCluyse, Michael E. McManus, and Masahiko Negishi 1690 Tibolone Is Metabolized by the 3a/3/3-Hydroxysteroid Dehydrogenase Activities of the Four Human Isozymes of the Aldo-Keto Reductase 1C Subfamily: Inversion of Stereospecificity with a A 5(10)-3-Ketosteroid Stephan Steckelbroeck, Yi Jin, Busola Oyesanmi, Helenius J. Kloosterboer, and Trevor M. Penning 1702 Long-Terra Exposure to Nicotine Modulates the Level and Activity of Acetylcholine Receptors in White Blood Cells of Smokers and Model Mice Anne Cormier, Yoav Paas, Roland Zini, Jean-Paul Tillement, Gilbert Lagrue, Jean-Pierre Changeux, and Regis Grailhe 1712 Transcriptional Regulation of the Human ju-Opioid Receptor Gene by Interleukin-6 Christine Borner, Ju'rgen Kraus, Helmut Schroder, Hermann Ammer, and Volker Hollt

1719 A Retinoic Acid Receptor j3/y-Selective Prodrug (tazarotene) Plus a Retinoid X Receptor Ligand Induces Extracellular Signal-Regulated Kinase Activation, Retinoblastoma Hypophosphorylation, G o Arrest, and Cell Differentiation Andrew Yen, Robert Fenning, Roshantha Chandraratna, Patricia Walker, and Susi Varvayanis 1727 Divergent Effects of the Purinoceptor Antagonists Suramin and Pyridoxal-5'-phosphate-6-(2'- naphthylazo-6'-nitro-4',8'-disulfonate) (PPNDS) on a-Amino-3-hydroxy-5-methyl-4- isoxazolepropionic Acid (AMPA) Receptors Erika Suzuki, Markus Kessler, Kyle Montgomery, and Amy C. Aral 1738