Human acyl-CoA:cholesterol acyltransferase (ACAT) and its potential as a target for pharmaceutical intervention against atherosclerosis.

Abstract

Acyl-CoA:cholesterol acyltransferase (ACAT) catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A. At the single-cell level, ACAT serves as a regulator of intracellular cholesterol homeostasis. In addition, ACAT supplies cholesteryl esters for lipoprotein assembly in the liver and small intestine. Under pathological conditions, the accumulation of cholesteryl esters produced by ACAT in macrophages contributes to foam cell formation, a hallmark of the early stage of atherosclerosis. Several reviews addressing various aspects of ACAT and ACAT inhibitors are available. This review briefly outlines the current knowledge on the biochemical properties of human ACATs, and then focuses on discussing the merit of ACAT as a drug target for pharmaceutical interventions against atherosclerosis.

• Authors: Catherine Chang, Ruhong Dong, Akira Miyazaki, Naomi Sakashita, Yi Zhang, Jay Liu, Michael Guo, Bo-Liang Li, Ta-Yuan Chang
• Journal: Acta biochimica et biophysica Sinica (Acta Biochim Biophys Sin (Shanghai)) Vol. 38 Issue 3 Pg. 151-6 (Mar 2006) ISSN: 1672-9145 [Print] China
• PMID: 16518538 (Publication Type: Journal Article, Review)

Chemical References

• Acyl Coenzyme A
• Cholesterol Esters
• Enzyme Inhibitors
• Hypolipidemic Agents
• Sterol O-Acyltransferase

Topics

• Acyl Coenzyme A (metabolism)
• Atherosclerosis (drug therapy, enzymology, prevention & control)
• Biological Transport
• Cell Membrane (metabolism)
• Cholesterol Esters (metabolism)
• Enzyme Inhibitors (pharmacology, therapeutic use)
• Homeostasis
• Humans
• Hypolipidemic Agents (pharmacology, therapeutic use)
• Immunohistochemistry
• Liver (drug effects, enzymology)
• Sterol O-Acyltransferase (antagonists & inhibitors, metabolism)