Table of Contents
August 12, 2004
Volume 47, Issue 17
Pages 4111-4338
About the Cover: Ribbon rendered illustration of the nuclear receptor heterodimer RXRα(cyan):PPARRγ (red) ligand binding domains bound with coactivator peptides (magenta) and agonist ligands (space-filling atoms where green is carbon, red is oxygen, and blue is nitrogen) (Haffner, C. D.; et al. J. Med. Chem. 2004, 47, 2010-2029).
Miniperspectives:Advances in Type 2 Diabetes
Novel “Second-Generation” Approaches for the Control of Type 2 Diabetes
David P. Rotella
pp 4111–4112Publication Date (Web): July 20, 2004 (Perspective)
DOI: 10.1021/jm030626a
Hi-Res PDFDiabetes Mellitus: Pathogenesis and Treatment Strategies
Jay S. Skyler
pp 4113–4117Publication Date (Web): July 20, 2004 (Perspective)
DOI: 10.1021/jm0306273
Peroxisome Proliferator-Activated Receptor α/γ Dual Agonists for the Treatment of Type 2 Diabetes
Brad R. Henke
pp 4118–4127Publication Date (Web): July 20, 2004 (Perspective)
DOI: 10.1021/jm030631e
Glucagon-like Peptide-1: The Basis of a New Class of Treatment for Type 2 Diabetes
Lotte Bjerre Knudsen
pp 4128–4134Publication Date (Web): July 20, 2004 (Perspective)
DOI: 10.1021/jm030630m
Dipeptidyl Peptidase IV Inhibitors for the Treatment of Diabetes
Ann E. Weber
pp 4135–4141Publication Date (Web): July 20, 2004 (Perspective)
DOI: 10.1021/jm030628v
Prospects for Inhibitors of Protein Tyrosine Phosphatase 1B as Antidiabetic Drugs
Rob Hooft van Huijsduijnen, Wolfgang H. B. Sauer, Agnes Bombrun, and Dominique Swinnen
pp 4142–4146Publication Date (Web): July 20, 2004 (Perspective)
DOI: 10.1021/jm030629n
Letters
Structure-Based Design, Synthesis, and Evaluation of Conformationally Constrained Mimetics of the Second Mitochondria-Derived Activator of Caspase That Target the X-Linked Inhibitor of Apoptosis Protein/Caspase-9 Interaction Site
Haiying Sun, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Liang Xu, York Tomita, Krzysztof Krajewski, Peter P. Roller, and Shaomeng Wang
pp 4147–4150Publication Date (Web): July 16, 2004 (Letter)
DOI: 10.1021/jm0499108
Rational Approaches to Discovery of Orally Active and Brain-Penetrable Quinazolinone Inhibitors of Poly(ADP-ribose)polymerase
Kouji Hattori, Yoshiyuki Kido, Hirofumi Yamamoto, Junya Ishida, Kazunori Kamijo, Kenji Murano, Mitsuru Ohkubo, Takayoshi Kinoshita, Akinori Iwashita, Kayoko Mihara, Syunji Yamazaki, Nobuya Matsuoka, Yoshinori Teramura, and Hiroshi Miyake
pp 4151–4154Publication Date (Web): July 16, 2004 (Letter)
DOI: 10.1021/jm0499256
Dopamine/Serotonin Receptor Ligands. 9.1 Oxygen-Containing Midsized Heterocyclic Ring Systems and Nonrigidized Analogues. A Step toward Dopamine D5 Receptor Selectivity
Thomas W. Wittig, Michael Decker, and Jochen Lehmann
pp 4155–4158Publication Date (Web): July 16, 2004 (Letter)
DOI: 10.1021/jm049720x
Bulky Nonproteinogenic Amino Acids Permit the Design of Very Small and Effective Cationic Antibacterial Peptides
Bengt Erik Haug, Wenche Stensen, Trine Stiberg, and John S. Svendsen
pp 4159–4162Publication Date (Web): July 16, 2004 (Letter)
DOI: 10.1021/jm049582b
A Nonpeptidic Sulfonamide Inhibits the p53−mdm2 Interaction and Activates p53-Dependent Transcription in mdm2-Overexpressing Cells
Peter S. Galatin and Donald J. Abraham
pp 4163–4165Publication Date (Web): July 21, 2004 (Letter)
DOI: 10.1021/jm034182u
Articles
Human Integrin αvβ5: Homology Modeling and Ligand Binding
Luciana Marinelli, Kay-E. Gottschalk, Axel Meyer, Ettore Novellino, and Horst Kessler
pp 4166–4177Publication Date (Web): July 10, 2004 (Article)
DOI: 10.1021/jm030635j
Combining Pharmacophore Search, Automated Docking, and Molecular Dynamics Simulations as a Novel Strategy for Flexible Docking. Proof of Concept: Docking of Arginine−Glycine−Aspartic Acid-like Compounds into the αvβ3 Binding Site
Nicolas Moitessier, Christophe Henry, Bernard Maigret, and Yves Chapleur
pp 4178–4187Publication Date (Web): July 20, 2004 (Article)
DOI: 10.1021/jm0311386
Validation of Automated Docking Programs for Docking and Database Screening against RNA Drug Targets
Carsten Detering and Gabriele Varani
pp 4188–4201Publication Date (Web): July 13, 2004 (Article)
DOI: 10.1021/jm030650o
Tricyclic Alkylamides as Melatonin Receptor Ligands with Antagonist or Inverse Agonist Activity
Valeria Lucini, Marilou Pannacci, Francesco Scaglione, Franco Fraschini, Sivia Rivara, Marco Mor, Fabrizio Bordi, Pier Vincenzo Plazzi, Gilberto Spadoni, Annalida Bedini, Giovanni Piersanti, Giuseppe Diamantini, and Giorgio Tarzia
pp 4202–4212Publication Date (Web): July 17, 2004 (Article)
DOI: 10.1021/jm040768k
Liver-Selective Glucocorticoid Antagonists: A Novel Treatment for Type 2 Diabetes
Thomas W. von Geldern, Noah Tu, Philip R. Kym, James T. Link, Hwan-Soo Jae, Chunqiu Lai, Theresa Apelqvist, Patrik Rhonnstad, Lars Hagberg, Konrad Koehler, Marlena Grynfarb, Annika Goos-Nilsson, Johnny Sandberg, Marie Österlund, Tomas Barkhem, Marie Höglund, Jiahong Wang, Steven Fung, Denise Wilcox, Phong Nguyen, Clarissa Jakob, Charles Hutchins, Mathias Färnegårdh, Björn Kauppi, Lars Öhman, and Peer B. Jacobson
pp 4213–4230Publication Date (Web): July 13, 2004 (Article)
DOI: 10.1021/jm0400045
Solution Structure of Amyloid β-Peptide (25−35) in Different Media
Anna M. D'Ursi, Maria R. Armenante, Remo Guerrini, Severo Salvadori, Giuseppe Sorrentino, and Delia Picone
pp 4231–4238Publication Date (Web): July 21, 2004 (Article)
DOI: 10.1021/jm040773o
Design, Synthesis, and Biological Evaluation of New Cyclic Disulfide Decapeptides That Inhibit the Binding of AP-1 to DNA
Keiichi Tsuchida, Hisaaki Chaki, Tadakazu Takakura, Junichi Yokotani, Yukihiko Aikawa, Shunichi Shiozawa, Hiroaki Gouda, and Shuichi Hirono
pp 4239–4246Publication Date (Web): July 21, 2004 (Article)
DOI: 10.1021/jm049890+
Full Text HTMLConcise Synthesis and Structure−Activity Relationships of Combretastatin A-4 Analogues, 1-Aroylindoles and 3-Aroylindoles, as Novel Classes of Potent Antitubulin Agents
Jing-Ping Liou, Yi-Ling Chang, Fu-Ming Kuo, Chun-Wei Chang, Huan-Yi Tseng, Chiung-Chiu Wang, Yung-Ning Yang, Jang-Yang Chang, Shiow-Ju Lee, and Hsing-Pang Hsieh
pp 4247–4257Publication Date (Web): July 17, 2004 (Article)
DOI: 10.1021/jm049802l
Three-Dimensional Quantitative Structure−Activity Relationship Analysis of a Set of Plasmodium falciparum Dihydrofolate Reductase Inhibitors Using a Pharmacophore Generation Approach
Marco Daniele Parenti, Sara Pacchioni, Anna Maria Ferrari, and Giulio Rastelli
pp 4258–4267Publication Date (Web): July 16, 2004 (Article)
DOI: 10.1021/jm040769c
2-(1-Adamantyl)-4-(thio)chromenone-6-carboxylic Acids: Potent Reversible Inhibitors of Human Steroid Sulfatase
Amarylla Horvath, Peter Nussbaumer, Barbara Wolff, and Andreas Billich
pp 4268–4276Publication Date (Web): July 09, 2004 (Article)
DOI: 10.1021/jm0407916
Phenoxyphenyl Pyridines as Novel State-Dependent, High-Potency Sodium Channel Inhibitors
Bin Shao, Sam Victory, Victor I. Ilyin, R. Richard Goehring, Qun Sun, Derk Hogenkamp, Diane D. Hodges, Khondaker Islam, Deyou Sha, Chongwu Zhang, Phong Nguyen, Silvia Robledo, George Sakellaropoulos, and Richard B. Carter
pp 4277–4285Publication Date (Web): July 16, 2004 (Article)
DOI: 10.1021/jm040048d
Identification of Structurally Diverse Growth Hormone Secretagogue Agonists by Virtual Screening and Structure−Activity Relationship Analysis of 2-Formylaminoacetamide Derivatives
Miyuki Shoda, Takeo Harada, Yuji Kogami, Ryuichi Tsujita, Hirotada Akashi, Hiroyuki Kouji, Florence L. Stahura, Ling Xue, and Jürgen Bajorath
pp 4286–4290Publication Date (Web): July 13, 2004 (Article)
DOI: 10.1021/jm040103i
Piperazine Derivatives of [1,2,4]Triazolo[1,5-a][1,3,5]triazine as Potent and Selective Adenosine A2a Receptor Antagonists
Chi B. Vu, Bo Peng, Gnanasambandam Kumaravel, Glenn Smits, Xiaowei Jin, Deepali Phadke, Thomas Engber, Carol Huang, Jennifer Reilly, Stacy Tam, Donna Grant, Gregg Hetu, Liqing Chen, Jianbo Zhang, and Russell C. Petter
pp 4291–4299Publication Date (Web): July 13, 2004 (Article)
DOI: 10.1021/jm0498405
Fluorescent Pirenzepine Derivatives as Potential Bitopic Ligands of the Human M1 Muscarinic Receptor
Chouaib Tahtaoui, Isabelle Parrot, Philippe Klotz, Fabrice Guillier, Jean-Luc Galzi, Marcel Hibert, and Brigitte Ilien
pp 4300–4315Publication Date (Web): July 16, 2004 (Article)
DOI: 10.1021/jm040800a
Tetramethylcyclopropyl Analogue of a Leading Antiepileptic Drug, Valproic Acid. Synthesis and Evaluation of Anticonvulsant Activity of Its Amide Derivatives
Eyal Sobol, Meir Bialer, and Boris Yagen
pp 4316–4326Publication Date (Web): July 20, 2004 (Article)
DOI: 10.1021/jm0498351
Zinc Ion Dependent B-Cell Epitope, Associated with Primary Sjogren's Syndrome, Resides within the Putative Zinc Finger Domain of Ro60kD Autoantigen: Physical and Immunologic Properties
John G. Routsias, Aggeliki Kosmopoulou, Athina Makri, Eugenia Panou-Pomonis, Constantinos Sakarellos, Maria Sakarellos-Daitsiotis, Haralampos M. Moutsopoulos, and Athanasios G. Tzioufas
pp 4327–4334Publication Date (Web): July 17, 2004 (Article)
DOI: 10.1021/jm049844+
Brief Articles
O-Alkoxyamidine Prodrugs of Furamidine: In Vitro Transport and Microsomal Metabolism as Indicators of in Vivo Efficacy in a Mouse Model of Trypanosoma brucei rhodesiense Infection
John H. Ansede, Mariappan Anbazhagan, Reto Brun, Judy D. Easterbrook, James Edwin Hall, and David W. Boykin
pp 4335–4338Publication Date (Web): July 16, 2004 (Brief Article)
DOI: 10.1021/jm030604o