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Acyl-CoA:diacylglycerol acyltransferase 1 (for DGAT1) and Acyl-CoA:diacylglycerol acyltransferase 2 (for DGAT2) (DGAT1, DGAT2)

Target
DGAT1, DGAT2
Molecular classification
Enzyme, Acyltransferase, Membrane-bound enzyme
01

Overview

Triglyceride biosynthesis enzymes are a class of enzymes that catalyze the formation of triglycerides from diacylglycerol and fatty acyl-CoA, a key step in lipid metabolism and energy storage[7][8][9]. The most well-characterized of these enzymes are DGAT1 and DGAT2, which mediate the final and committed step in triglyceride synthesis[8][9]. These enzymes are essential for the proper storage of energy in adipocytes and hepatocytes, regulation of lipid droplet formation, and the assembly of lipoproteins for lipid transport in blood[7][8][9]. Dysregulation or inhibition of these enzymes has been explored for therapeutic intervention in metabolic diseases such as obesity and non-alcoholic fatty liver disease but presents safety challenges due to their central role in energy metabolism[8][9]. The phrase refers to a functional group of enzymes and not a unique molecule; the most pharmacologically relevant and studied individual targets within this group are DGAT1 and DGAT2. For structured data or drug discovery, it is crucial to map to the most specific single molecular entity (e.g., DGAT1 or DGAT2)[8][9].

Other names
diacylglycerol acyltransferasetriacylglycerol synthaseDGAT enzymestriglyceride synthaseTAG synthase
02

Mechanism of action

Inhibition of triglyceride synthesis via acyl-CoA:diacylglycerol acyltransferase blockade Reduced chylomicron and VLDL synthesis Decreased intestinal lipid absorption

03

Biological functions

Triglyceride biosynthesisEnergy storageLipid droplet formationLipoprotein assembly
04

Disease associations

ObesityType 2 diabetesNon-alcoholic fatty liver disease (NAFLD)Cardiovascular diseaseLipodystrophy
05

Safety considerations

Fat malabsorption (diarrhea with DGAT1 inhibition)SteatorrheaGastrointestinal discomfortPotential interference with fat-soluble vitamin absorptionEffects on hormonal regulation (leptin/adiponectin)
06

Interacting drugs

Pradigastat (DGAT1 inhibitor)

3 more in the full profile.

07

Biomarkers

Hepatic triglyceride content (imaging or biopsy)Plasma triglyceride levelsLipoprotein profiles (VLDL, chylomicron)

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