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Hit-to-Lead Optimization and Discovery of 5-((5-([1,1'-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase.
Lan P, Romero FA, Wodka D, Kassick AJ, Dang Q, Gibson T, Cashion D, Zhou G, Chen Y, Zhang X, Zhang A, Li Y, Trujillo ME, Shao Q, Wu M, Xu S, He H, MacKenna D, Staunton J, Chapman KT, Weber A, Sebhat IK, Makara GM. Lan P, et al. Among authors: zhou g. J Med Chem. 2017 Nov 9;60(21):9040-9052. doi: 10.1021/acs.jmedchem.7b01344. Epub 2017 Oct 25. J Med Chem. 2017. PMID: 29035567
Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase.
Feng D, Biftu T, Romero FA, Kekec A, Dropinski J, Kassick A, Xu S, Kurtz MM, Gollapudi A, Shao Q, Yang X, Lu K, Zhou G, Kemp D, Myers RW, Guan HP, Trujillo ME, Li C, Weber A, Sebhat IK. Feng D, et al. Among authors: zhou g. ACS Med Chem Lett. 2017 Dec 1;9(1):39-44. doi: 10.1021/acsmedchemlett.7b00417. eCollection 2018 Jan 11. ACS Med Chem Lett. 2017. PMID: 29348809 Free PMC article.
Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy.
Myers RW, Guan HP, Ehrhart J, Petrov A, Prahalada S, Tozzo E, Yang X, Kurtz MM, Trujillo M, Gonzalez Trotter D, Feng D, Xu S, Eiermann G, Holahan MA, Rubins D, Conarello S, Niu X, Souza SC, Miller C, Liu J, Lu K, Feng W, Li Y, Painter RE, Milligan JA, He H, Liu F, Ogawa A, Wisniewski D, Rohm RJ, Wang L, Bunzel M, Qian Y, Zhu W, Wang H, Bennet B, LaFranco Scheuch L, Fernandez GE, Li C, Klimas M, Zhou G, van Heek M, Biftu T, Weber A, Kelley DE, Thornberry N, Erion MD, Kemp DM, Sebhat IK. Myers RW, et al. Among authors: zhou g. Science. 2017 Aug 4;357(6350):507-511. doi: 10.1126/science.aah5582. Epub 2017 Jul 13. Science. 2017. PMID: 28705990
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Wang S, Xu S, Chen HS, Tong X, Tong V, Mitra K, Kumar S, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Chen X, Zhang B, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: zhou g. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3398-404. doi: 10.1016/j.bmcl.2009.05.036. Epub 2009 May 18. Bioorg Med Chem Lett. 2009. PMID: 19481932
(2R)-2-ethylchromane-2-carboxylic acids: discovery of novel PPARalpha/gamma dual agonists as antihyperglycemic and hypolipidemic agents.
Koyama H, Miller DJ, Boueres JK, Desai RC, Jones AB, Berger JP, MacNaul KL, Kelly LJ, Doebber TW, Wu MS, Zhou G, Wang PR, Ippolito MC, Chao YS, Agrawal AK, Franklin R, Heck JV, Wright SD, Moller DE, Sahoo SP. Koyama H, et al. Among authors: zhou g. J Med Chem. 2004 Jun 3;47(12):3255-63. doi: 10.1021/jm030621d. J Med Chem. 2004. PMID: 15163205
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Shen HC, Ding FX, Deng Q, Xu S, Chen HS, Tong X, Tong V, Zhang X, Chen Y, Zhou G, Pai LY, Alonso-Galicia M, Zhang B, Roy S, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: zhou g. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5314-20. doi: 10.1016/j.bmcl.2009.07.138. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19682899
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Ogawa AK, Bunte EV, Mal R, Lan P, Sun Z, Crespo A, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Jochnowitz N, Ma X, Pan Y, Brown P, Zamlynny B, Bateman T, Leung D, Xu L, Tong X, Liu K, Crook M, Sinclair P. Ogawa AK, et al. Among authors: zhou g. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2866-2869. doi: 10.1016/j.bmcl.2016.04.052. Epub 2016 Apr 20. Bioorg Med Chem Lett. 2016. PMID: 27161805
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.
Shen HC, Ding FX, Wang S, Deng Q, Zhang X, Chen Y, Zhou G, Xu S, Chen HS, Tong X, Tong V, Mitra K, Kumar S, Tsai C, Stevenson AS, Pai LY, Alonso-Galicia M, Chen X, Soisson SM, Roy S, Zhang B, Tata JR, Berger JP, Colletti SL. Shen HC, et al. Among authors: zhou g. J Med Chem. 2009 Aug 27;52(16):5009-12. doi: 10.1021/jm900725r. J Med Chem. 2009. PMID: 19645482
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