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AMG 837: a potent, orally bioavailable GPR40 agonist.
Houze JB, Zhu L, Sun Y, Akerman M, Qiu W, Zhang AJ, Sharma R, Schmitt M, Wang Y, Liu J, Liu J, Medina JC, Reagan JD, Luo J, Tonn G, Zhang J, Lu JY, Chen M, Lopez E, Nguyen K, Yang L, Tang L, Tian H, Shuttleworth SJ, Lin DC. Houze JB, et al. Among authors: zhang aj, zhang j. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70. doi: 10.1016/j.bmcl.2011.10.118. Epub 2011 Nov 6. Bioorg Med Chem Lett. 2012. PMID: 22217876
Activation of FFA1 mediates GLP-1 secretion in mice. Evidence for allosterism at FFA1.
Xiong Y, Swaminath G, Cao Q, Yang L, Guo Q, Salomonis H, Lu J, Houze JB, Dransfield PJ, Wang Y, Liu JJ, Wong S, Schwandner R, Steger F, Baribault H, Liu L, Coberly S, Miao L, Zhang J, Lin DC, Schwarz M. Xiong Y, et al. Among authors: zhang j. Mol Cell Endocrinol. 2013 Apr 30;369(1-2):119-29. doi: 10.1016/j.mce.2013.01.009. Epub 2013 Feb 9. Mol Cell Endocrinol. 2013. PMID: 23403053
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Brown SP, Dransfield PJ, Vimolratana M, Jiao X, Zhu L, Pattaropong V, Sun Y, Liu J, Luo J, Zhang J, Wong S, Zhuang R, Guo Q, Li F, Medina JC, Swaminath G, Lin DC, Houze JB. Brown SP, et al. Among authors: zhang j. ACS Med Chem Lett. 2012 Aug 15;3(9):726-30. doi: 10.1021/ml300133f. eCollection 2012 Sep 13. ACS Med Chem Lett. 2012. PMID: 24900539 Free PMC article.
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Wang Y, Liu JJ, Dransfield PJ, Zhu L, Wang Z, Du X, Jiao X, Su Y, Li AR, Brown SP, Kasparian A, Vimolratana M, Yu M, Pattaropong V, Houze JB, Swaminath G, Tran T, Nguyen K, Guo Q, Zhang J, Zhuang R, Li F, Miao L, Bartberger MD, Correll TL, Chow D, Wong S, Luo J, Lin DC, Medina JC. Wang Y, et al. Among authors: zhang j. ACS Med Chem Lett. 2013 May 7;4(6):551-5. doi: 10.1021/ml300427u. eCollection 2013 Jun 13. ACS Med Chem Lett. 2013. PMID: 24900707 Free PMC article.
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
Du X, Dransfield PJ, Lin DC, Wong S, Wang Y, Wang Z, Kohn T, Yu M, Brown SP, Vimolratana M, Zhu L, Li AR, Su Y, Jiao X, Liu JJ, Swaminath G, Tran T, Luo J, Zhuang R, Zhang J, Guo Q, Li F, Connors R, Medina JC, Houze JB. Du X, et al. Among authors: zhang j. ACS Med Chem Lett. 2014 Feb 3;5(4):384-9. doi: 10.1021/ml4005123. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900845 Free PMC article.
Optimization of GPR40 Agonists for Type 2 Diabetes.
Liu JJ, Wang Y, Ma Z, Schmitt M, Zhu L, Brown SP, Dransfield PJ, Sun Y, Sharma R, Guo Q, Zhuang R, Zhang J, Luo J, Tonn GR, Wong S, Swaminath G, Medina JC, Lin DC, Houze JB. Liu JJ, et al. Among authors: zhang j. ACS Med Chem Lett. 2014 Feb 6;5(5):517-21. doi: 10.1021/ml400501x. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900872 Free PMC article.
Discovery of the imidazole-derived GPR40 agonist AM-3189.
Ma Z, Lin DC, Sharma R, Liu J, Zhu L, Li AR, Kohn T, Wang Y, Liu JJ, Bartberger MD, Medina JC, Zhuang R, Li F, Zhang J, Luo J, Wong S, Tonn GR, Houze JB. Ma Z, et al. Among authors: zhang j. Bioorg Med Chem Lett. 2016 Jan 1;26(1):15-20. doi: 10.1016/j.bmcl.2015.11.050. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26620255
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