Identification and preliminary characterization of a potent, safe, and orally efficacious inhibitor of acyl-CoA:diacylglycerol acyltransferase 1.
暂无分享,去创建一个
Steven C. Cullen | P. Hajduk | A. Souers | J. Segreti | A. King | D. Beno | D. Beno | C. Collins | K. Marsh | P. Kym | M. Voorbach | S. Mittelstadt | B. Dayton | R. Reilly | M. Brune | B. Cox | S. Brodjian | A. Judd | V. Yeh | Y. Lau | Xiaojun Wang | T. M. Hansen | R. Klix | K. Larson | E. Stoner | M. Dhaon | M. Rozema | Ju Gao | H. Falls | Gang Zhao | N. Grihalde | H. D. Falls | D. Plata | Xili Xin | C. A. Collins | Martin J. Voorbach | T. Hansen | Kennan C. Marsh | T. M. Hansen | Andrew S. Judd | Steven C. Cullen | Andrew J. King | Russel C. Klix | Yau Y. Lau | Eric J. Stoner | Bryan F. Cox
[1] Eliot Sugarman,et al. Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. , 2011, ACS medicinal chemistry letters.
[2] C. Rondinone,et al. Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. , 2011, Journal of medicinal chemistry.
[3] A. Souers,et al. In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. , 2010, European journal of pharmacology.
[4] A. Souers,et al. Diacylglycerol Acyltransferase 1 Inhibition Lowers Serum Triglycerides in the Zucker Fatty Rat and the Hyperlipidemic Hamster , 2009, Journal of Pharmacology and Experimental Therapeutics.
[5] A. Turnbull,et al. Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. , 2009, Journal of medicinal chemistry.
[6] Robert V Farese,et al. Thematic review series: glycerolipids. DGAT enzymes and triacylglycerol biosynthesis. , 2008, Journal of lipid research.
[7] A. Souers,et al. Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. , 2008, Journal of medicinal chemistry.
[8] J. T. Metz,et al. Ligand efficiency indices as guideposts for drug discovery. , 2005, Drug discovery today.
[9] A. Nassar,et al. Improving the decision-making process in the structural modification of drug candidates: enhancing metabolic stability. , 2004, Drug discovery today.
[10] Robert V Farese,et al. Role of adipocyte-derived factors in enhancing insulin signaling in skeletal muscle and white adipose tissue of mice lacking Acyl CoA:diacylglycerol acyltransferase 1. , 2004, Diabetes.
[11] Robert V Farese,et al. DGAT1 Is Not Essential for Intestinal Triacylglycerol Absorption or Chylomicron Synthesis* , 2002, The Journal of Biological Chemistry.
[12] Robert V Farese,et al. Increased insulin and leptin sensitivity in mice lacking acyl CoA:diacylglycerol acyltransferase 1. , 2002, The Journal of clinical investigation.
[13] Robert V Farese,et al. Cloning of DGAT2, a Second Mammalian Diacylglycerol Acyltransferase, and Related Family Members* , 2001, The Journal of Biological Chemistry.
[14] Robert V Farese,et al. Obesity resistance and multiple mechanisms of triglyceride synthesis in mice lacking Dgat , 2000, Nature Genetics.
[15] Robert V Farese,et al. Identification of a gene encoding an acyl CoA:diacylglycerol acyltransferase, a key enzyme in triacylglycerol synthesis. , 1998, Proceedings of the National Academy of Sciences of the United States of America.
[16] Robert V Farese,et al. Analysis of energy expenditure at different ambient temperatures in mice lacking DGAT1. , 2003, American journal of physiology. Endocrinology and metabolism.
[17] J. McGarry. Banting lecture 2001: dysregulation of fatty acid metabolism in the etiology of type 2 diabetes. , 2002, Diabetes.