Cholesteryl ester transfer protein: pharmacological inhibition for the modulation of plasma cholesterol levels and promising target for the prevention of atherosclerosis.
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.
Ruggeri
Roger B
RB
Department of Medicinal Chemistry, Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. roger_b_ruggeri@groton.pfizer.com
D001161:Arteriosclerosis / Q000097:blood* / Q000378:metabolism / Q000517:prevention & control; D002318:Cardiovascular Diseases / Q000517:prevention & control; D002352:Carrier Proteins / Q000187:drug effects / Q000378:metabolism*; D002784:Cholesterol / Q000097:blood* / Q000378:metabolism; D053480:Cholesterol Ester Transfer Proteins; D016503:Drug Delivery Systems; D006023:Glycoproteins / Q000172:deficiency / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D000960:Hypolipidemic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D008074:Lipoproteins / Q000097:blood / Q000378:metabolism; D016032:Randomized Controlled Trials as Topic
C506642:CETP protein, human; D002352:Carrier Proteins; D053480:Cholesterol Ester Transfer Proteins; D006023:Glycoproteins; D000960:Hypolipidemic Agents; D008074:Lipoproteins; D002784:Cholesterol