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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
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.
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.
Edmondson SD, Mastracchio A, Cox JM, Eiermann GJ, He H, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Xu S, Zhu B, Thornberry NA, Roy RS, Weber AE. Edmondson SD, et al. Among authors: he h. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4097-101. doi: 10.1016/j.bmcl.2009.06.011. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19539471
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
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
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.
Caldwell CG, Chen P, He J, Parmee ER, Leiting B, Marsilio F, Patel RA, Wu JK, Eiermann GJ, Petrov A, He H, Lyons KA, Thornberry NA, Weber AE. Caldwell CG, et al. Among authors: he h, he j. Bioorg Med Chem Lett. 2004 Mar 8;14(5):1265-8. doi: 10.1016/j.bmcl.2003.12.040. Bioorg Med Chem Lett. 2004. PMID: 14980678
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Biftu T, Feng D, Qian X, Liang GB, Kieczykowski G, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Scapin G, Patel S, Gao YD, Singh S, Wu J, Zhang X, Thornberry NA, Weber AE. Biftu T, et al. Among authors: he h. Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. doi: 10.1016/j.bmcl.2006.09.099. Epub 2006 Oct 5. Bioorg Med Chem Lett. 2007. PMID: 17055272
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
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