Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that facilitates the transfer of cholesteryl esters from the atheroprotective high density lipoprotein (HDL) to the proatherogenic low density lipoprotein cholesterol (LDL) and very low density lipoprotein cholesterol (VLDL) leading to lower levels of HDL but raising the levels of proatherogenic LDL and VLDL. CETP inhibitors are a class of drugs that targets the CETP enzyme to significantly increase serum HDL-C and decrease LDL-C levels. Inhibition of CETP is considered a potential approach to treat dyslipidemia.
Alterations of CETP activity levels can be caused by single-base polymorphisms as well as by alternative splicing. Several common variants in CETP have been reported to be associated with variation in plasma lipid levels, CAD risk and/or CETP mass/activity. The rare genetic variants in the CETP gene also contribute to the phenotypic variation of HDL-C in the general population.