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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: he h. 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
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE. Biftu T, et al. Among authors: he h, he j. J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24660890
Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.
Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe JT, Gao YD, Scapin G, Cox J, Doss G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Weber AE, Yan Y, Roy RS, Biftu T. Chen P, et al. Among authors: he h. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5767-71. doi: 10.1016/j.bmcl.2015.10.070. Epub 2015 Oct 30. Bioorg Med Chem Lett. 2015. PMID: 26546218
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: he h. Science. 2017 Aug 4;357(6350):507-511. doi: 10.1126/science.aah5582. Epub 2017 Jul 13. Science. 2017. PMID: 28705990
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
Graham TH, Liu W, Verras A, Sebhat IK, Xiong Y, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xiao J, Xie D, Xu S, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Among authors: he h. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2811-7. doi: 10.1016/j.bmcl.2012.02.075. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22444683
Pharmacological AMPK activation induces transcriptional responses congruent to exercise in skeletal and cardiac muscle, adipose tissues and liver.
Muise ES, Guan HP, Liu J, Nawrocki AR, Yang X, Wang C, Rodríguez CG, Zhou D, Gorski JN, Kurtz MM, Feng D, Leavitt KJ, Wei L, Wilkening RR, Apgar JM, Xu S, Lu K, Feng W, Li Y, He H, Previs SF, Shen X, van Heek M, Souza SC, Rosenbach MJ, Biftu T, Erion MD, Kelley DE, Kemp DM, Myers RW, Sebhat IK. Muise ES, et al. Among authors: he h. PLoS One. 2019 Feb 27;14(2):e0211568. doi: 10.1371/journal.pone.0211568. eCollection 2019. PLoS One. 2019. PMID: 30811418 Free PMC article.
(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE. Edmondson SD, et al. Among authors: he h, he j. J Med Chem. 2006 Jun 15;49(12):3614-27. doi: 10.1021/jm060015t. J Med Chem. 2006. PMID: 16759103
Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.
Xu J, Wei L, Mathvink RJ, Edmondson SD, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE. Xu J, et al. Among authors: he h. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5373-7. doi: 10.1016/j.bmcl.2006.07.061. Epub 2006 Aug 17. Bioorg Med Chem Lett. 2006. PMID: 16919457
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