Current Topics in Medicinal Chemistry

Author(s): Roger B. Ruggeri

DOI: 10.2174/1568026053544506

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Cholesteryl Ester Transfer Protein: Pharmacological Inhibition for the Modulation of Plasma Cholesterol Levels and Promising Target for the Prevention of Atherosclerosis.

Page: [257 - 264] Pages: 8

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Abstract

Cholesteryl ester transfer protein (CETP) facilitates the exchange of neutral lipids (such as cholesteryl esters and triglycerides) between anti-atherogenic HDL particles and pro-atherogenic VLDL and LDL particles in human plasma. Individuals possessing a genetic deficiency for CETP have higher HDL cholesterol and lower LDL cholesterol and may have a reduced risk for developing cardiovascular disease. Small molecule inhibitors of CETP are being developed that would appear to provide a beneficial change in lipoprotein profile. However, randomized clinical trials are ultimately required to determine whether CETP inhibition will afford a reduction in cardiovascular events.

Keywords: low-density lipoprotein cholesterol (ldl-c), coronary heart disease (chd), reverse cholesterol transport(rct), inflammatory processes, vascular endothelial cells, glycopeptide, phospholipids