Target intelligence / Profile preview

Acyl-CoA:1,2-diacylglycerol acyltransferase (DGAT)

Target
DGAT
Molecular classification
Enzyme, Acyltransferase, Membrane protein
01

Overview

Acyl-CoA:1,2-diacylglycerol acyltransferase (DGAT) is an integral membrane enzyme that catalyzes the final and only committed step in the biosynthesis of triacylglycerol (TAG). There are two main isoforms in mammals, DGAT1 and DGAT2. DGAT plays a central role in cellular glycerolipid metabolism and is essential for physiological processes such as intestinal fat absorption, lipoprotein assembly, adipose tissue formation, and lactation. Disruption or inhibition of these enzymes affects lipid droplet formation, fatty acid oxidation rates, lipogenic gene expression, and overall lipid homeostasis—making them potential therapeutic targets for obesity, diabetes mellitus type II, dyslipidemia/metabolic syndrome, atherosclerosis/cardiovascular disease.

Other names
Diacylglycerol acyltransferaseDGAT1DGAT2
02

Mechanism of action

Inhibition of DGAT1 or DGAT2 reduces triacylglycerol synthesis.

03

Biological functions

Triacylglycerol biosynthesisLipid storageFat absorptionLipoprotein assemblyGlycerolipid metabolism
04

Disease associations

ObesityDiabetes Mellitus Type IIDyslipidemiaMetabolic syndromeAtherosclerosisCardiovascular disease
05

Safety considerations

Potential for off-target effectsEffects on unrelated receptors or ion channelsDisruption of lipid homeostasis
06

Interacting drugs

DGAT1 inhibitors

2 more in the full profile.

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