| Literature DB >> 18183944 |
Gang Zhao1, Andrew J Souers, Martin Voorbach, H Doug Falls, Brian Droz, Sevan Brodjian, Yau Yi Lau, Rajesh R Iyengar, Ju Gao, Andrew S Judd, Seble H Wagaw, Matthew M Ravn, Kenneth M Engstrom, John K Lynch, Mathew M Mulhern, Jennifer Freeman, Brian D Dayton, Xiaojun Wang, Nelson Grihalde, Dennis Fry, David W A Beno, Kennan C Marsh, Zhi Su, Gilbert J Diaz, Christine A Collins, Hing 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.Entities:
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Year: 2008 PMID： 18183944 DOI： 10.1021/jm7013887
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446