Increased level of serum cholesterol (hyperlipidemia) is the most significant risk factor for the development of
atherosclerosis. Cholesterol levels are affected by factors such as rate of endogenous cholesterol synthesis, biliary
cholesterol excretion and dietary cholesterol absorption. Acyl CoA: Cholesterol O-acyl transferases (ACAT) are a small
family of enzymes that catalyze cholesterol esterification and cholesterol absorption in intestinal mucosal cells and
maintain the cholesterol homeostasis in the blood. Inhibition of the ACAT enzymes is one of the attractive targets to treat
hyperlipidemia. Literature survey shows that structurally diverse compounds possess ACAT inhibitory properties. In this
review, a comprehensive presentation of the literature on diverse ACAT inhibitors has been given.
Keywords: Cholesterol, Hyperlipidemia, Atherosclerosis, Acyl CoA: Cholesterol O-acyl transferase (ACAT), Cholesterol
esterification, ACAT inhibitors.
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