Discovery of a novel class of PPARdelta partial agonists.
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Shearer BG, Patel HS, Billin AN, Way JM, Winegar DA, Lambert MH, Xu RX, Leesnitzer LM, Merrihew RV, Huet S, Willson TM
Discovery of a novel class of PPARdelta partial agonists.
Bioorg Med Chem Lett. 2008 Sep 15;18(18):5018-22. doi: 10.1016/j.bmcl.2008.08.011. Epub 2008 Aug 9.
- PubMed ID
- 18722772 [ View in PubMed]
- 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.