Inhibition of cholesteryl ester transfer protein activity: a new therapeutic approach to raising high-density lipoprotein.
High-density lipoprotein (HDL) cholesterol levels are inversely associated with risk of atherosclerotic cardiovascular disease (ASCVD), leading to the concept that pharmacologic therapy to raise HDL cholesterol levels may reduce ASCVD risk. There is substantial interest in the concept of inhibition of the cholesteryl ester transfer protein (CETP) as a novel strategy for raising HDL cholesterol levels, as well as reducing levels of atherogenic lipoproteins. This article reviews the physiology of CETP in lipoprotein metabolism and the data in animals and humans that are relevant to the question of whether CETP inhibition may some day be part of the clinical armamentarium for treating dyslipidemia and atherosclerotic vascular disease.
Center for Experimental Therapeutics and Department of Medicine, University of Pennsylvania School of Medicine, 654 BRB II/III, 421 Curie Boulevard, Philadelphia, PA 19104, USA. rader@mail.med.upenn.edu
Daniel J
DJ
Rader
D000818:Animals; D001161:Arteriosclerosis / Q000188:drug therapy / Q000209:etiology; D002318:Cardiovascular Diseases / Q000188:drug therapy / Q000209:etiology; D002352:Carrier Proteins / Q000235:genetics / Q000494:pharmacology* / Q000627:therapeutic use; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL / Q000187:drug effects* / Q000378:metabolism; D006023:Glycoproteins / Q000172:deficiency / Q000235:genetics / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D006949:Hyperlipidemias / Q000150:complications / Q000188:drug therapy; D051379:Mice; D011110:Polymorphism, Genetic
C506642:CETP protein, human; D002352:Carrier Proteins; D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL; D006023:Glycoproteins