Diacylglycerol acyltransferases (DGATs) catalyze the final step in triglyceride synthesis. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. Amidepsine A is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits DGAT activity (IC50 = 10.2 μM in rat liver microsomes). It inhibits triacylglycerol formation in Raji cells with an IC50 value of 15.5 μM.
