DGAT

Diacylglycerol acyltransferase (DGAT) inhibitors block the final step of triglyceride synthesis. DGAT enzymes transfer a fatty acyl group from acyl-coenzyme A (acyl-CoA) onto diacylglycerol. DGAT1 was identified in 1998 through its sequence similarity to cholesterol acyltransferases. DGAT2, cloned in 2001, shares no sequence similarity with DGAT1 and belongs to a separate gene family. Both enzymes are studied in models of dietary fat absorption, hepatic lipid storage and obesity. A 922500, PF-04620110, AZD7687 and pradigastat are DGAT1 inhibitors, whereas PF-06424439 inhibits DGAT2. Comparing the two classes helps separate the roles of the isoforms in intestine, liver and adipose tissue.

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