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Updated: Aug 12, 2026
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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 series of PPAR gamma/delta dual agonists via solid-phase parallel synthesis
K G Liu1, M H Lambert, L M Leesnitzer
1Nuclear Receptor Discovery Research, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. kevin_liu@stromix.com
Bioorganic & Medicinal Chemistry Letters
|October 26, 2001
Abstract:
We have developed a general solid-phase synthesis for identification of PPAR ligands. Synthesis of a 480-member library led to the identification of a potent PPAR gamma/delta dual agonist 23. Compound 23 showed good plasma exposure in rats and demonstrated antihyperglycemic and antihyperlipidemic efficacy in diabetic fatty Zucker rats.
