[HTML][HTML] Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
J Cao, Y Zhou, H Peng, X Huang, S Stahler… - Journal of Biological …, 2011 - ASBMB
Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) is one of two known DGAT enzymes that
catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as
well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for
the treatment of obesity and type 2 diabetes. Here we characterize a tool DGAT1 inhibitor
compound, T863. We found that T863 is a potent inhibitor for both human and mouse
DGAT1 in vitro, which acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1 …
catalyze the final step in triglyceride synthesis. Findings from genetically modified mice as
well as pharmacological studies suggest that inhibition of DGAT1 is a promising strategy for
the treatment of obesity and type 2 diabetes. Here we characterize a tool DGAT1 inhibitor
compound, T863. We found that T863 is a potent inhibitor for both human and mouse
DGAT1 in vitro, which acts on the acyl-CoA binding site of DGAT1 and inhibits DGAT1 …