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Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.
Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Zhou C, Lin S, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger JP, Mills SG, Thornberry NA, Yang L, Howard AD. Tan CP, et al. Among authors: einstein m. Diabetes. 2008 Aug;57(8):2211-9. doi: 10.2337/db08-0130. Epub 2008 May 13. Diabetes. 2008. PMID: 18477808 Free PMC article.
Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.
Zhou C, Tang C, Chang E, Ge M, Lin S, Cline E, Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger J, Howard AD, Thornberry N, Mills SG, Yang L. Zhou C, et al. Among authors: einstein m. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1298-301. doi: 10.1016/j.bmcl.2009.10.052. Epub 2009 Oct 15. Bioorg Med Chem Lett. 2010. PMID: 20064714
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators.
Liu W, Lau F, Liu K, Wood HB, Zhou G, Chen Y, Li Y, Akiyama TE, Castriota G, Einstein M, Wang C, McCann ME, Doebber TW, Wu M, Chang CH, McNamara L, McKeever B, Mosley RT, Berger JP, Meinke PT. Liu W, et al. Among authors: einstein m. J Med Chem. 2011 Dec 22;54(24):8541-54. doi: 10.1021/jm201061j. Epub 2011 Nov 28. J Med Chem. 2011. PMID: 22070604
Highly functionalized 7-azaindoles as selective PPAR gamma modulators.
Debenham SD, Chan A, Lau FW, Liu W, Wood HB, Lemme K, Colwell L, Habulihaz B, Akiyama TE, Einstein M, Doebber TW, Sharma N, Wang CF, Wu M, Berger JP, Meinke PT. Debenham SD, et al. Among authors: einstein m. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4798-801. doi: 10.1016/j.bmcl.2008.07.103. Epub 2008 Jul 30. Bioorg Med Chem Lett. 2008. PMID: 18701276
Discovery of (2R)-2-(3-{3-[(4-Methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid (MK-0533): a novel selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus with a reduced potential to increase plasma and extracellular fluid volume.
Acton JJ 3rd, Akiyama TE, Chang CH, Colwell L, Debenham S, Doebber T, Einstein M, Liu K, McCann ME, Moller DE, Muise ES, Tan Y, Thompson JR, Wong KK, Wu M, Xu L, Meinke PT, Berger JP, Wood HB. Acton JJ 3rd, et al. Among authors: einstein m. J Med Chem. 2009 Jul 9;52(13):3846-54. doi: 10.1021/jm900097m. J Med Chem. 2009. PMID: 19507861
Selective glucocorticoid receptor nonsteroidal ligands completely antagonize the dexamethasone mediated induction of enzymes involved in gluconeogenesis and glutamine metabolism.
Einstein M, Greenlee M, Rouen G, Sitlani A, Santoro J, Wang C, Pandit S, Mazur P, Smalera I, Weaver AP, Zeng YY, Ge L, Kelly T, Paiva T, Geissler W, Mosley RT, Williamson J, Ali A, Balkovec J, Harris G. Einstein M, et al. J Steroid Biochem Mol Biol. 2004 Dec;92(5):345-56. doi: 10.1016/j.jsbmb.2004.10.009. Epub 2005 Jan 21. J Steroid Biochem Mol Biol. 2004. PMID: 15698539
246 results