HDL, ABC transporters, and cholesterol efflux: implications for the treatment of atherosclerosis

Cell Metab. 2008 May;7(5):365-75. doi: 10.1016/j.cmet.2008.03.001.


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.

Publication types

  • Review

MeSH terms

  • ATP-Binding Cassette Transporters / metabolism*
  • Animals
  • Atherosclerosis / metabolism
  • Atherosclerosis / therapy*
  • Cholesterol / metabolism*
  • Humans
  • Lipoproteins, HDL / metabolism*


  • ATP-Binding Cassette Transporters
  • Lipoproteins, HDL
  • Cholesterol