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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 D is a fungal metabolite isolated from the culture broth of Humicola sp. FO-2942 that inhibits DGAT activity (IC50 = 17.5 µM in rat liver microsomes).1 It inhibits triacylglycerol formation in Raji cells with an IC50 value of 2.8 µM.1
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Tomoda, H., Ito, M., Tabata, N., et al. Amidepsines, inhibitors of diacylglycerol acyltransferase produced by Humicola sp. FO-