Target intelligence / Profile preview

Acyl-CoA Diacylglycerol Acyltransferase (DGAT)

Target
DGAT
Molecular classification
Enzyme, Acyltransferase, Membrane protein
01

Overview

Acyl-CoA:diacylglycerol acyltransferase (DGAT) is a microsomal enzyme that catalyzes the terminal and only committed step in triacylglycerol (TAG) synthesis, using diacylglycerol and fatty acyl CoA as substrates. This reaction is essential for the formation of TAGs, which are the primary storage form of energy in eukaryotic cells. DGAT plays a central role in lipid metabolism including intestinal fat absorption, lipoprotein assembly/secretion, adipose tissue formation/storage, lactation, and overall energy homeostasis. Pharmacological inhibition of DGAT enzymes—especially DGAT1—is being explored for treating metabolic disorders.

Other names
Acyl-CoA:diacylglycerol acyltransferaseDiacylglycerol acyltransferaseDGAT1DGAT2DGAT3WSDs
02

Mechanism of action

Inhibition of DGAT activity, specifically acyl-CoA binding.

03

Biological functions

Triacylglycerol biosynthesisLipid metabolismIntestinal fat absorptionLipoprotein assembly/secretionAdipose tissue formation/storageLactationEnergy homeostasis
04

Disease associations

ObesityType 2 diabetes mellitusHepatic steatosis (fatty liver)HyperlipidemiaCardiovascular disease
05

Safety considerations

Potential toxicity from DGAT inhibitors
06

Interacting drugs

T863

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