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Page 1
Glucagon receptor antagonism induces increased cholesterol absorption.
Guan HP, Yang X, Lu K, Wang SP, Castro-Perez JM, Previs S, Wright M, Shah V, Herath K, Xie D, Szeto D, Forrest G, Xiao JC, Palyha O, Sun LP, Andryuk PJ, Engel SS, Xiong Y, Lin S, Kelley DE, Erion MD, Davis HR, Wang L. Guan HP, et al. Among authors: yang x. J Lipid Res. 2015 Nov;56(11):2183-95. doi: 10.1194/jlr.M060897. Epub 2015 Sep 15. J Lipid Res. 2015. PMID: 26373568 Free PMC article.
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.
Xiong Y, Guo J, Candelore MR, Liang R, Miller C, Dallas-Yang Q, Jiang G, McCann PE, Qureshi SA, Tong X, Xu SS, Shang J, Vincent SH, Tota LM, Wright MJ, Yang X, Zhang BB, Tata JR, Parmee ER. Xiong Y, et al. Among authors: yang x. J Med Chem. 2012 Jul 12;55(13):6137-48. doi: 10.1021/jm300579z. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22708876
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: yang x. 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: yang x. PLoS One. 2019 Feb 27;14(2):e0211568. doi: 10.1371/journal.pone.0211568. eCollection 2019. PLoS One. 2019. PMID: 30811418 Free PMC article.
Physiological Expression of AMPKγ2RG Mutation Causes Wolff-Parkinson-White Syndrome and Induces Kidney Injury in Mice.
Yang X, Mudgett J, Bou-About G, Champy MF, Jacobs H, Monassier L, Pavlovic G, Sorg T, Herault Y, Petit-Demoulière B, Lu K, Feng W, Wang H, Ma LJ, Askew R, Erion MD, Kelley DE, Myers RW, Li C, Guan HP. Yang X, et al. J Biol Chem. 2016 Nov 4;291(45):23428-23439. doi: 10.1074/jbc.M116.738591. Epub 2016 Sep 12. J Biol Chem. 2016. PMID: 27621313 Free PMC article.
A novel glucagon receptor antagonist inhibits glucagon-mediated biological effects.
Qureshi SA, Rios Candelore M, Xie D, Yang X, Tota LM, Ding VD, Li Z, Bansal A, Miller C, Cohen SM, Jiang G, Brady E, Saperstein R, Duffy JL, Tata JR, Chapman KT, Moller DE, Zhang BB. Qureshi SA, et al. Among authors: yang x. Diabetes. 2004 Dec;53(12):3267-73. doi: 10.2337/diabetes.53.12.3267. Diabetes. 2004. PMID: 15561959
Discovery of potent, orally active benzimidazole glucagon receptor antagonists.
Kim RM, Chang J, Lins AR, Brady E, Candelore MR, Dallas-Yang Q, Ding V, Dragovic J, Iliff S, Jiang G, Mock S, Qureshi S, Saperstein R, Szalkowski D, Tamvakopoulos C, Tota L, Wright M, Yang X, Tata JR, Chapman K, Zhang BB, Parmee ER. Kim RM, et al. Among authors: yang x. Bioorg Med Chem Lett. 2008 Jul 1;18(13):3701-5. doi: 10.1016/j.bmcl.2008.05.072. Epub 2008 May 22. Bioorg Med Chem Lett. 2008. PMID: 18539028
Discovery of N-aryl-2-acylindole human glucagon receptor antagonists.
Sinz C, Bittner A, Brady E, Candelore M, Dallas-Yang Q, Ding V, Jiang G, Lin Z, Qureshi S, Salituro G, Saperstein R, Shang J, Szalkowski D, Tota L, Vincent S, Wright M, Xu S, Yang X, Zhang B, Tata J, Kim R, Parmee ER. Sinz C, et al. Among authors: yang x. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7124-30. doi: 10.1016/j.bmcl.2011.09.105. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22030028
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Shen DM, Brady EJ, Candelore MR, Dallas-Yang Q, Ding VD, Feeney WP, Jiang G, McCann ME, Mock S, Qureshi SA, Saperstein R, Shen X, Tong X, Tota LM, Wright MJ, Yang X, Zheng S, Chapman KT, Zhang BB, Tata JR, Parmee ER. Shen DM, et al. Among authors: yang x. Bioorg Med Chem Lett. 2011 Jan 1;21(1):76-81. doi: 10.1016/j.bmcl.2010.11.074. Epub 2010 Nov 21. Bioorg Med Chem Lett. 2011. PMID: 21147532
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