Target intelligence / Profile preview

Diglyceride acyltransferase (DGAT)

Target
DGAT
Molecular classification
Enzyme, Transferase, Membrane protein
01

Overview

Diglyceride acyltransferase (DGAT) is a membrane-bound enzyme that catalyzes the final and only committed step in the biosynthesis of triglycerides from diacylglycerol and fatty acyl-CoA. This reaction is essential for energy storage as fat, intestinal absorption of dietary fats, adipose tissue formation, milk production, and overall lipid homeostasis. There are two main isoforms in mammals—DGAT1 and DGAT2—which perform similar biochemical functions but have distinct tissue distributions and regulatory properties. Disruption or pharmacological inhibition of these enzymes affects body fat accumulation, energy balance, lactation ability, skin integrity, and may influence susceptibility to obesity-related diseases. Because of its central role in triglyceride metabolism—and its impact on conditions like obesity—DGAT is considered a promising therapeutic target for metabolic disorders[1][2][4][5].

Other names
Diacylglycerol acyltransferaseO-acyltransferaseAcyl-CoA:diacylglycerol acyltransferaseTriacylglycerol synthaseDGAT1 (isoform)DGAT2 (isoform)
02

Mechanism of action

Inhibition of DGAT reduces triglyceride synthesis and fat absorption/storage (primarily via blocking the final step in triacylglycerol biosynthesis)

03

Biological functions

Triglyceride (triacylglycerol) synthesisLipid metabolismEnergy storage regulationIntestinal fat absorptionLipoprotein assembly
04

Disease associations

ObesityMetabolic syndrome/insulin resistanceCardiovascular disease risk (via plasma triglycerides)Lipodystrophy and related lipid storage disorders
05

Safety considerations

Potential for impaired lactation with strong inhibition (as seen in knockout mice)Possible skin barrier defects or lipopenia with excessive inhibition
06

Interacting drugs

Experimental DGAT1 inhibitors for obesity and metabolic diseases

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