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.
Mini-Reviews in Medicinal Chemistry
Title:ACAT Inhibitors: The Search for Novel Cholesterol Lowering Agents
Volume: 13 Issue: 8
Author(s): Palash Pal, Hardik Gandhi, Rajani Giridhar and Mange Ram Yadav
Affiliation:
Keywords: Cholesterol, Hyperlipidemia, Atherosclerosis, Acyl CoA: Cholesterol O-acyl transferase (ACAT), Cholesterol esterification, ACAT inhibitors.
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.
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Cite this article as:
Pal Palash, Gandhi Hardik, Giridhar Rajani and Yadav Mange Ram, ACAT Inhibitors: The Search for Novel Cholesterol Lowering Agents, Mini-Reviews in Medicinal Chemistry 2013; 13 (8) . https://dx.doi.org/10.2174/1389557511313080007
DOI https://dx.doi.org/10.2174/1389557511313080007 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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