Literature DB >> 12699745

Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity.

Marcos L Sznaidman1, Curt D Haffner, Patrick R Maloney, Adam Fivush, Esther Chao, Donna Goreham, Michael L Sierra, Christelle LeGrumelec, H Eric Xu, Valerie G Montana, Millard H Lambert, Timothy M Willson, William R Oliver, Daniel D Sternbach.   

Abstract

We report the synthesis and biological activity of a new series of small molecule agonists of the human Peroxisome Proliferator-Activated Receptor delta (PPARdelta). Several hits were identified from our original libraries containing lipophilic carboxylic acids. Optimization of these hits by structure-guided design led to 7k (GW501516) and 7l (GW0742), which shows an EC(50) of 1.1 nM against PPARdelta with 1000-fold selectivity over the other human subtypes.

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Year:  2003        PMID： 12699745     DOI： 10.1016/s0960-894x(03)00207-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.940


  103 in total

Review 1.  Peroxisome proliferator-activated receptor-delta, a regulator of oxidative capacity, fuel switching and cholesterol transport.

Authors:  C Fürnsinn; T M Willson; B Brunmair
Journal:  Diabetologia       Date:  2006-11-22       Impact factor: 10.122

2.  PPARdelta agonism inhibits skeletal muscle PDC activity, mitochondrial ATP production and force generation during prolonged contraction.

Authors:  Dumitru Constantin-Teodosiu; David J Baker; Despina Constantin; Paul L Greenhaff
Journal:  J Physiol       Date:  2008-11-10       Impact factor: 5.182

Review 3.  Neuroprotective mechanisms of peroxisome proliferator-activated receptor agonists in Alzheimer's disease.

Authors:  Rupinder K Sodhi; Nirmal Singh; Amteshwar S Jaggi
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2011-05-24       Impact factor: 3.000

4.  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

5.  Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs.

Authors:  Kelly Teske; Premchendar Nandhikonda; Jonathan W Bogart; Belaynesh Feleke; Preetpal Sidhu; Nina Yuan; Joshua Preston; Robin Goy; Leggy A Arnold
Journal:  J Biomol Res Ther       Date:  2014

6.  Peroxisome proliferator-activated receptor beta/delta expression and activation in lung cancer.

Authors:  Tetyana V Pedchenko; Adriana L Gonzalez; DingZhi Wang; Raymond N DuBois; Pierre P Massion
Journal:  Am J Respir Cell Mol Biol       Date:  2008-06-19       Impact factor: 6.914

7.  PPAR-delta in Vascular Pathophysiology.

Authors:  Nanping Wang
Journal:  PPAR Res       Date:  2009-01-06       Impact factor: 4.964

8.  Peroxisome proliferator-activated receptor beta activation promotes myonuclear accretion in skeletal muscle of adult and aged mice.

Authors:  C Giordano; A S Rousseau; N Wagner; C Gaudel; J Murdaca; C Jehl-Piétri; B Sibille; P A Grimaldi; P Lopez
Journal:  Pflugers Arch       Date:  2009-05-05       Impact factor: 4.458

9.  PPAR-delta senses and orchestrates clearance of apoptotic cells to promote tolerance.

Authors:  Lata Mukundan; Justin I Odegaard; Christine R Morel; Jose E Heredia; Julia W Mwangi; Roberto R Ricardo-Gonzalez; Y P Sharon Goh; Alex Red Eagle; Shannon E Dunn; Jennifer U H Awakuni; Khoa D Nguyen; Lawrence Steinman; Sara A Michie; Ajay Chawla
Journal:  Nat Med       Date:  2009-10-18       Impact factor: 87.241

10.  Regulation of oligodendrocyte progenitor cell maturation by PPARδ: effects on bone morphogenetic proteins.

Authors:  Maria Vittoria Simonini; Paul E Polak; Anne I Boullerne; Jeffrey M Peters; Jill C Richardson; Douglas L Feinstein
Journal:  ASN Neuro       Date:  2010-01-15       Impact factor: 5.200
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