Target intelligence / Profile preview

Acyl-CoA Cholesterol Acyltransferase (ACAT)

Target
ACAT
Molecular classification
Enzyme, Acyltransferase
01

Overview

Acyl-CoA cholesterol acyltransferase (ACAT), also known as sterol O-acyltransferase (SOAT), is a membrane-bound enzyme that catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty acyl-CoA. This reaction is crucial for cellular cholesterol homeostasis, as it converts potentially toxic free cholesterol into a storage form—cholesteryl esters—which are sequestered in cytoplasmic lipid droplets or incorporated into lipoproteins. There are two main isoenzymes in mammals: ACAT1 (SOAT1), ubiquitously expressed and primarily involved in intracellular cholesterol homeostasis, and ACAT2 (SOAT2), mainly in the liver and intestine, playing a key role in lipoprotein assembly. ACAT activity is implicated in diseases like atherosclerosis, Alzheimer's, and cancer, making it a potential therapeutic target.

Other names
Sterol O-acyltransferaseSOATSOAT1SOAT2ACAT1ACAT2
02

Mechanism of action

Inhibition of cholesterol esterification

03

Biological functions

Cholesterol esterificationIntracellular cholesterol homeostasisLipoprotein assemblySteroid hormone synthesisCholesterol storage
04

Disease associations

AtherosclerosisAlzheimer's DiseaseCancer
05

Safety considerations

Potential for off-target effects due to ubiquitous expression (ACAT1)Complex role in lipid metabolism requires careful monitoring
06

Interacting drugs

ACAT inhibitors (unspecified)
07

Biomarkers

Cholesteryl ester levelsOxysterol levels

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