A Cholesterol Ester Transfer Protein Inhibitor Attenuates Atherosclerosis in Rabbits
Document Type
Article
Publication Date
11-22-2000
Journal / Book Title
Nature
Abstract
Cholesteryl ester transfer protein (CETP) is a plasma protein that mediates the exchange of cholesteryl ester in high-density lipoprotein (HDL) for triglyceride in very low density lipoprotein (VLDL)1,2. This process decreases the level of anti-atherogenic HDL cholesterol and increases pro-atherogenic VLDL and low density lipoprotein (LDL) cholesterol, so CETP is potentially atherogenic3,4,5,6,7,8,9. On the other hand, CETP could also be anti-atherogenic10,11,12,13,14, because it participates in reverse cholesterol transport (transfer of cholesterol from peripheral cells through the plasma to the liver)15. Because the role of CETP in atherosclerosis remains unclear, we have attempted to develop a potent and specific CETP inhibitor. Here we describe CETP inhibitors that form a disulphide bond with CETP, and present one such inhibitor (JTT-705) that increases HDL cholesterol, decreases non-HDL cholesterol and inhibits the progression of atherosclerosis in rabbits. Our findings indicate that CETP may be atherogenic in vivo and that JTT-705 may be a potential anti-atherogenic drug.
DOI
10.1038/35018119
Montclair State University Digital Commons Citation
Rotella, David, "A Cholesterol Ester Transfer Protein Inhibitor Attenuates Atherosclerosis in Rabbits" (2000). Department of Chemistry and Biochemistry Faculty Scholarship and Creative Works. 541.
https://digitalcommons.montclair.edu/chem-biochem-facpubs/541