Acyl-CoA Cholesterol Acyltransferase 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.
Mechanism of Action
Inhibition of cholesterol esterification
Biological Functions
Disease Associations
Safety Considerations
- Potential for off-target effects due to ubiquitous expression (ACAT1)
- Complex role in lipid metabolism requires careful monitoring
Interacting Drugs
Associated Biomarkers
Biomarker |
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Cholesteryl ester levels |
Oxysterol levels |