Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor
Journal of Medicinal Chemistry2008Vol. 51(3), pp. 380–383
Citations Over TimeTop 10% of 2008 papers
Gang Zhao, Andrew J. Souers, Martin J. Voorbach, H. Doug Falls, Brian A. Droz, Sevan Brodjian, Yau Yi Lau, Rajesh R. Iyengar, Ju Gao, Andrew S. Judd, Seble Wagaw, Matthew M. Ravn, Kenneth M. Engstrom, J.A. Lynch, Mathew M. Mulhern, Jennifer C. Freeman, Brian D. Dayton, Xiaojun Wang, Nelson Grihalde, Dennis G. Fry, David W. A. Beno, Kennan C. Marsh, Zhi Su, Gilbert Diaz, Christine A. Collins, Hing L. Sham, Regina M. Reilly, Michael E. Brune, Philip R. Kym
Abstract
A highly potent and selective DGAT-1 inhibitor was identified and used in rodent models of obesity and postprandial chylomicron excursion to validate DGAT-1 inhibition as a novel approach for the treatment of metabolic diseases. Specifically, compound 4a conferred weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depleted serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice.
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