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Page 1
Discovery of a novel class of PPARdelta partial agonists.
Shearer BG, Patel HS, Billin AN, Way JM, Winegar DA, Lambert MH, Xu RX, Leesnitzer LM, Merrihew RV, Huet S, Willson TM. Shearer BG, et al. Bioorg Med Chem Lett. 2008 Sep 15;18(18):5018-22. doi: 10.1016/j.bmcl.2008.08.011. Epub 2008 Aug 9. Bioorg Med Chem Lett. 2008. PMID: 18722772
Co-crystal structure guided array synthesis of PPARgamma inverse agonists.
Trump RP, Cobb JE, Shearer BG, Lambert MH, Nolte RT, Willson TM, Buckholz RG, Zhao SM, Leesnitzer LM, Iannone MA, Pearce KH, Billin AN, Hoekstra WJ. Trump RP, et al. Among authors: shearer bg. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3916-20. doi: 10.1016/j.bmcl.2007.04.111. Epub 2007 May 18. Bioorg Med Chem Lett. 2007. PMID: 17533125
Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.
Shearer BG, Wiethe RW, Ashe A, Billin AN, Way JM, Stanley TB, Wagner CD, Xu RX, Leesnitzer LM, Merrihew RV, Shearer TW, Jeune MR, Ulrich JC, Willson TM. Shearer BG, et al. J Med Chem. 2010 Feb 25;53(4):1857-61. doi: 10.1021/jm900464j. J Med Chem. 2010. PMID: 20128594
Phenoxyacetic acids as PPARδ partial agonists: synthesis, optimization, and in vivo efficacy.
Evans KA, Shearer BG, Wisnoski DD, Shi D, Sparks SM, Sternbach DD, Winegar DA, Billin AN, Britt C, Way JM, Epperly AH, Leesnitzer LM, Merrihew RV, Xu RX, Lambert MH, Jin J. Evans KA, et al. Among authors: shearer bg. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2345-50. doi: 10.1016/j.bmcl.2011.02.077. Epub 2011 Mar 15. Bioorg Med Chem Lett. 2011. PMID: 21414782
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist.
Sime M, Allan AC, Chapman P, Fieldhouse C, Giblin GM, Healy MP, Lambert MH, Leesnitzer LM, Lewis A, Merrihew RV, Rutter RA, Sasse R, Shearer BG, Willson TM, Xu RX, Virley DJ. Sime M, et al. Among authors: shearer bg. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5568-72. doi: 10.1016/j.bmcl.2011.06.088. Epub 2011 Jun 29. Bioorg Med Chem Lett. 2011. PMID: 21798739
32 results