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Page 1
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC. Sun D, et al. Among authors: houze jb. J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24456472
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. 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
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D. Gonzalez AZ, et al. Among authors: houze jb. J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4. J Med Chem. 2014. PMID: 24548297
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: houze jb. 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
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
Gonzalez AZ, Li Z, Beck HP, Canon J, Chen A, Chow D, Duquette J, Eksterowicz J, Fox BM, Fu J, Huang X, Houze J, Jin L, Li Y, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Sun D, Medina JC. Gonzalez AZ, et al. J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27. J Med Chem. 2014. PMID: 24601644
Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.
Rew Y, Sun D, Yan X, Beck HP, Canon J, Chen A, Duquette J, Eksterowicz J, Fox BM, Fu J, Gonzalez AZ, Houze J, Huang X, Jiang M, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Saiki AY, Shaffer P, Wang YC, Wortman S, Yakowec P, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Rew Y, et al. J Med Chem. 2014 Dec 26;57(24):10499-511. doi: 10.1021/jm501550p. Epub 2014 Dec 4. J Med Chem. 2014. PMID: 25384157
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: houze jb. 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: houze jb. 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.
Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.
Yu M, Lizarzaburu M, Motani A, Fu Z, Du X, Liu JJ, Jiao X, Lai S, Fan P, Fu A, Liu Q, Murakoshi M, Nara F, Oda K, Okuyama R, Reagan JD, Watanabe N, Yamazaki M, Xiong Y, Zhang Y, Zhuang R, Lin DC, Houze JB, Medina JC, Li L. Yu M, et al. Among authors: houze jb. ACS Med Chem Lett. 2013 May 1;4(9):829-34. doi: 10.1021/ml4000854. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900757 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: houze jb. 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.
31 results