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CETP inhibitors block cholesteryl ester transfer protein, which moves lipids between plasma lipoproteins. Cholesteryl ester transfer protein (CETP) carries cholesteryl esters from high-density lipoprotein (HDL) to apolipoprotein B-containing particles in exchange for triglycerides. The human complementary DNA (cDNA) for the protein was cloned and sequenced in 1987. In 1990, a common CETP gene mutation was linked to raised HDL levels in Japanese families. A 2007 crystal structure revealed a long hydrophobic tunnel in the protein that holds four bound lipid molecules. Torcetrapib, anacetrapib and evacetrapib are inhibitors used to study lipoprotein remodeling, while dalcetrapib modulates CETP through a different binding mode. Obicetrapib is a more recent inhibitor that is also used in lipoprotein research.
