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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

ACAT Inhibitors: The Search for Novel Cholesterol Lowering Agents

Author(s): Palash Pal, Hardik Gandhi, Rajani Giridhar and Mange Ram Yadav

Volume 13, Issue 8, 2013

Page: [1195 - 1219] Pages: 25

DOI: 10.2174/1389557511313080007

Price: $65

Abstract

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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