Acyl CoA: diacylglycerol acyltransferase1 (DGAT1) is a ubiquitously-expressed multifunctional enzyme that catalyzes the terminal step of triacylglycerol biosynthesis.  One of the signature pharmacodynamic effects of DGAT1 inhibition is the suppression of circulating triglycerides following oral ingestion of lipid, owing to the high intestinal expression of DGAT1 and its role in dietary fat absorption.  We describe here medicinal chemistry efforts to identify several unique DGAT1 inhibitor profiles.  Preclinical and clinical data which support the development of DGAT1 inhibitors will be presented.

Discovery of a DGAT1 inhibitor with robust suppression of postprandial triglyceride levels in humans

243rd National Meeting (2012)

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