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Updated: Aug 10, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis
P J Brown1, L W Stuart, K P Hurley
1GlaxoSmithKline, Research Triangle Park, NC 27709-3398, USA. pjb5890@gsk.com
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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