Literature DB >> 11354382

Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.

P J Brown1, L W Stuart, K P Hurley, M C Lewis, D A Winegar, J G Wilson, W O Wilkison, O R Ittoop, T M Willson.   

Abstract

Using solid-phase, parallel-array synthesis, a series of urea-substituted thioisobutyric acids was synthesized and assayed for activity on the human PPAR subtypes. GW7647 (3) was identified as a potent human PPARalpha agonist with approximately 200-fold selectivity over PPARgamma and PPARdelta, and potent lipid-lowering activity in animal models of dyslipidemia. GW7647 (3) will be a valuable chemical tool for studying the biology of PPARalpha in human cells and animal models of disease.

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Year:  2001        PMID： 11354382     DOI： 10.1016/s0960-894x(01)00188-3

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  39 in total

1.  Peroxisome proliferator-activated receptors target family landscape: a chemometrical approach to ligand selectivity based on protein binding site analysis.

Authors:  Bernard Pirard
Journal:  J Comput Aided Mol Des       Date:  2003-11       Impact factor: 3.686

Review 2.  Recent advances in metabolic imaging.

Authors:  Robert J Gropler
Journal:  J Nucl Cardiol       Date:  2013-12       Impact factor: 5.952

3.  Peroxisome proliferator-activated receptor-α activation promotes macrophage reverse cholesterol transport through a liver X receptor-dependent pathway.

Authors:  Kazuhiro Nakaya; Junichiro Tohyama; Snehal U Naik; Hiroyuki Tanigawa; Colin MacPhee; Jeffrey T Billheimer; Daniel J Rader
Journal:  Arterioscler Thromb Vasc Biol       Date:  2011-03-24       Impact factor: 8.311

4.  Lipidomics identifies a requirement for peroxisomal function during influenza virus replication.

Authors:  Lukas Bahati Tanner; Charmaine Chng; Xue Li Guan; Zhengdeng Lei; Steven G Rozen; Markus R Wenk
Journal:  J Lipid Res       Date:  2014-05-27       Impact factor: 5.922

5.  Selective and cell-active inhibitors of the USP1/ UAF1 deubiquitinase complex reverse cisplatin resistance in non-small cell lung cancer cells.

Authors:  Junjun Chen; Thomas S Dexheimer; Yongxing Ai; Qin Liang; Mark A Villamil; James Inglese; David J Maloney; Ajit Jadhav; Anton Simeonov; Zhihao Zhuang
Journal:  Chem Biol       Date:  2011-11-23

6.  Peroxisome proliferator-activated receptor α mediates acute effects of palmitoylethanolamide on sensory neurons.

Authors:  Iryna A Khasabova; Yee Xiong; Lia G Coicou; Daniele Piomelli; Virginia Seybold
Journal:  J Neurosci       Date:  2012-09-12       Impact factor: 6.167

7.  Differential inhibition of macrophage foam-cell formation and atherosclerosis in mice by PPARalpha, beta/delta, and gamma.

Authors:  Andrew C Li; Christoph J Binder; Alejandra Gutierrez; Kathleen K Brown; Christine R Plotkin; Jennifer W Pattison; Annabel F Valledor; Roger A Davis; Timothy M Willson; Joseph L Witztum; Wulf Palinski; Christopher K Glass
Journal:  J Clin Invest       Date:  2004-12       Impact factor: 14.808

8.  The PPARalpha/p16INK4a pathway inhibits vascular smooth muscle cell proliferation by repressing cell cycle-dependent telomerase activation.

Authors:  Florence Gizard; Takashi Nomiyama; Yue Zhao; Hannes M Findeisen; Elizabeth B Heywood; Karrie L Jones; Bart Staels; Dennis Bruemmer
Journal:  Circ Res       Date:  2008-09-25       Impact factor: 17.367

Review 9.  Humanized mouse lines and their application for prediction of human drug metabolism and toxicological risk assessment.

Authors:  Connie Cheung; Frank J Gonzalez
Journal:  J Pharmacol Exp Ther       Date:  2008-08-05       Impact factor: 4.030

10.  Sulindac derivatives that activate the peroxisome proliferator-activated receptor gamma but lack cyclooxygenase inhibition.

Authors:  Andrew S Felts; Brianna S Siegel; Shiu M Young; Christopher W Moth; Terry P Lybrand; Andrew J Dannenberg; Lawrence J Marnett; Kotha Subbaramaiah
Journal:  J Med Chem       Date:  2008-07-30       Impact factor: 7.446
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