HDL, ABC transporters, and cholesterol efflux: implications for the treatment of atherosclerosis.
High-density lipoprotein (HDL) has been identified as a potential target in the treatment of atherosclerotic vascular disease. The failure of torcetrapib, an inhibitor of cholesteryl ester transfer protein (CETP) that markedly increased HDL levels in a clinical trial, has called into doubt the efficacy of HDL elevation. Recent analysis suggests that failure may have been caused by off-target toxicity and that HDL is functional and promotes regression of atherosclerosis. New studies highlight the central importance of the ATP-binding cassette (ABC) transporters ABCA1 and ABCG1 in reducing macrophage foam cell formation, inflammation, and atherosclerosis. A variety of approaches to increasing HDL may eventually be successful in treating atherosclerosis.
Tall
Alan R
AR
Division of Molecular Medicine, Department of Medicine, Columbia University, New York, NY 10032, USA.
Yvan-Charvet
Laurent
L
Terasaka
Naoki
N
Pagler
Tamara
T
Wang
Nan
N
D018528:ATP-Binding Cassette Transporters / Q000378:metabolism*; D000818:Animals; D050197:Atherosclerosis / Q000378:metabolism / Q000628:therapy*; D002784:Cholesterol / Q000378:metabolism*; D006801:Humans; D008075:Lipoproteins, HDL / Q000378:metabolism*
D018528:ATP-Binding Cassette Transporters; D008075:Lipoproteins, HDL; D002784:Cholesterol