title: Therapies targeting exogenous cholesterol uptake: new insights and controversies.
abstract: 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.
authors.affiliation: Clinical Professor, Director of Preventive Cardiology, The University of Chicago Pritzker School of Medicine, 515 North State Street, Suite 2700, Chicago, IL 60654, USA. michaeldavidson@radiantresearch.com
authors.forename: Michael H
authors.initials: MH
authors.lastname: Davidson
mesh_terms: D018528:ATP-Binding Cassette Transporters / Q000493:pharmacokinetics; D000818:Animals; D000924:Anticholesteremic Agents / Q000494:pharmacology*; D050197:Atherosclerosis / Q000188:drug therapy* / Q000378:metabolism; D001384:Azetidines / Q000494:pharmacology; D001647:Bile Acids and Salts / Q000378:metabolism; D001692:Biological Transport / Q000187:drug effects; D002784:Cholesterol / Q000493:pharmacokinetics*; D008076:Cholesterol, HDL / Q000378:metabolism; D055808:Drug Discovery / Q000639:trends; D000069438:Ezetimibe; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D008659:Metabolic Diseases / Q000188:drug therapy* / Q000378:metabolism; D051379:Mice; D058990:Molecular Targeted Therapy / Q000639:trends*; D012855:Sitosterols / Q000493:pharmacokinetics; D002785:Sterol O-Acyltransferase / Q000493:pharmacokinetics; D000097587:Sterol O-Acyltransferase 2
chemical_list: D018528:ATP-Binding Cassette Transporters; D000924:Anticholesteremic Agents; D001384:Azetidines; D001647:Bile Acids and Salts; D002784:Cholesterol; D008076:Cholesterol, HDL; D000069438:Ezetimibe; D012855:Sitosterols; D002785:Sterol O-Acyltransferase; D000097587:Sterol O-Acyltransferase 2