, Volume 13, Issue 1, pp 95-100
Date: 29 Dec 2010

Therapies Targeting Exogenous Cholesterol Uptake: New Insights and Controversies

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Exogenous cholesterol uptake involves a complex process in the intestines for the absorption of cholesterol and bile acids. This process is regulated by intestinal nuclear transcription factors such as LXR that affect sterol transporters NPC1L1, ABCG5/G8, and ABCG1, and enzymes such as ACAT-2. Plant sterol/stanols, ezetimibe, and bile acid sequestrants have a variety of effects on these various transporters, and new insights into their mechanism(s) of action have provided a plethora of exciting targets for metabolic diseases, dyslipidemia, and atherosclerosis.