Journey Through Cholesteryl Ester Transfer Protein Inhibition

Journey through cholesteryl ester transfer protein inhibition: from bench to bedside.

Plasma cholesteryl ester transfer protein.

The plasma lipoproteins are continuously remodeled during their transit through the plasma compartment, owing to the action of lipid metabolizing enzymes and lipid transfer processes. These activities have a major effect on the composition, size, and concentration of the lipoproteins. Lipid transfer processes involving neutral lipids and phospholipids are mediated by specialized plasma proteins...

Cholesteryl Ester Transfer Protein Inhibition Is Not Yet Dead--Pro.

Cholesteryl ester transfer protein (CETP) transfers cholesteryl esters from nonatherogenic high-density lipoproteins to potentially proatherogenic non-high-density lipoprotein fractions. Human genetic studies and human cohort studies have concluded that CETP gene polymorphisms associated with decreased CETP activity are accompanied by a significantly lower risk of atherosclerotic cardiovascular...

Cholesteryl ester transfer protein inhibition: effect on reverse cholesterol transport?

Statins, inhibitors of the key enzyme in the biosynthesis of cholesterol (ie, 3-hydroxy-3-methylglutaryl [HMG]coenzyme A [CoA] reductase), are widely used as the prevailing strategy to combat atherosclerosis through reducing LDL cholesterol levels. Large-scale clinical trials have shown that statins markedly reduce coronary events.1,2 A meta-analysis of 22 studies enrolling nearly 70 000 indivi...

Inhibition of cholesteryl ester transfer protein by fungal metabolites, L681,512.

The cholesteryl ester transfer protein (CETP) promotes exchange and transfer of neutral lipids such as cholesteryl ester (CE) and triacylglycerol (TG) between plasma lipoproteins. Evidence is accumulating for involvement of CETP in atherosclerosis1'2). Therefore, CETP is expected as a novel target of inhibition for anti-atherosclerotic agents. In the course of our screening for CETP inhibitors ...