Literature DB >> 18722772

Discovery of a novel class of PPARdelta partial agonists.

Barry G Shearer1, Hari S Patel, Andrew N Billin, James M Way, Deborah A Winegar, Millard H Lambert, Robert X Xu, Lisa M Leesnitzer, Raymond V Merrihew, Stephane Huet, Timothy M Willson.   

Abstract

Anthranilic acid GW9371 was identified as a novel class of PPARdelta partial agonist through high-throughput screening. The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARdelta target genes CPT1a and PDK4 in skeletal muscle cells.

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Year:  2008        PMID: 18722772     DOI: 10.1016/j.bmcl.2008.08.011

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


  6 in total

Review 1.  Activation of PPARδ: from computer modelling to biological effects.

Authors:  Shirin Kahremany; Ariela Livne; Arie Gruzman; Hanoch Senderowitz; Shlomo Sasson
Journal:  Br J Pharmacol       Date:  2014-12-15       Impact factor: 8.739

Review 2.  Migraine signaling pathways: amino acid metabolites that regulate migraine and predispose migraineurs to headache.

Authors:  Roger Gregory Biringer
Journal:  Mol Cell Biochem       Date:  2022-04-28       Impact factor: 3.842

3.  Regulation of tissue-specific carboxylesterase expression by pregnane x receptor and constitutive androstane receptor.

Authors:  Chenshu Xu; Xinkun Wang; Jeff L Staudinger
Journal:  Drug Metab Dispos       Date:  2009-04-09       Impact factor: 3.922

Review 4.  Current and Future Treatments in the Fight Against Non-Alcoholic Fatty Liver Disease.

Authors:  Benoit Smeuninx; Ebru Boslem; Mark A Febbraio
Journal:  Cancers (Basel)       Date:  2020-06-28       Impact factor: 6.639

5.  Structure-based virtual screening and discovery of New PPARδ/γ dual agonist and PPARδ and γ agonists.

Authors:  Vinicius G Maltarollo; Marie Togashi; Alessandro S Nascimento; Kathia M Honorio
Journal:  PLoS One       Date:  2015-03-13       Impact factor: 3.240

6.  Discovering highly selective and diverse PPAR-delta agonists by ligand based machine learning and structural modeling.

Authors:  Benny Da'adoosh; David Marcus; Anwar Rayan; Fred King; Jianwei Che; Amiram Goldblum
Journal:  Sci Rep       Date:  2019-01-31       Impact factor: 4.379

  6 in total

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