Intravascular metabolism of the cholesteryl ester moiety of rat plasma lipoproteins.

Treatment of cholesterol-fed male hamsters kept on a diet of purina chow with beta beta'-methyl-substituted hexadecanedioic acid (MEDICA 16) resulted in a progressive hypocholesterolaemic effect, amounting to a 50% decrease in the cholesterol content of all plasma lipoproteins. The decrease in plasma cholesterol could be accounted for by activation of plasma-cholesterol efflux through the liver into the bile mediated by MEDICA 16-induced (a) increase of the number of liver LDL receptors, (b) activation of liver neutral cholesteryl ester hydrolase with a concomitant inhibition of liver acyl-CoA cholesterol acyltransferase, resulting in shifting of the liver cholesteryl ester/free-cholesterol cycle in the direction of free cholesterol, and (c) activation of cholesterol efflux from the liver into the bile. The increase in bile cholesterol output was accompanied by an increase in bile phospholipids but not in bile acids. In contrast with rats, MEDICA 16-treatment of male hamsters did not result in a hypotriacylglycerolaemic effect, inhibition of lipogenesis, nor in a substantial decrease in plasma apolipoprotein C-III content.

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Cholesteryl Ester Transfer Protein Reaction between Plasma Lipoproteins

The Journal of Biochemistry ◽

10.1093/oxfordjournals.jbchem.a022087 ◽

1998 ◽

Vol 124 (1) ◽

pp. 237-243 ◽

Cited By ~ 6

Author(s):

L. A. Main ◽

K. Okumura-Noji ◽

T. Ohnishi ◽

S. Yokoyama

Keyword(s):

Cholesteryl Ester ◽

Cholesteryl Ester Transfer Protein ◽

Plasma Lipoproteins ◽

Transfer Protein ◽

Protein Reaction

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4.P.349 Effect of alcohol-induced changes in plasma lipoproteins and lipids on cholesteryl ester transfer

Atherosclerosis ◽

10.1016/s0021-9150(97)89877-2 ◽

1997 ◽

Vol 134 (1-2) ◽

pp. 370

Author(s):

M.J. Liinamaa ◽

Y.A. Kesäniemi ◽

M.J. Savolainen

Keyword(s):

Cholesteryl Ester ◽

Plasma Lipoproteins ◽

Induced Changes

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Cholesteryl Ester Transfer Protein Inhibitors

Journal of Cardiovascular Pharmacology and Therapeutics ◽

10.1177/1074248416662349 ◽

2016 ◽

Vol 22 (2) ◽

pp. 99-104 ◽

Cited By ~ 8

Author(s):

Julian Hardy McLain ◽

Andrew Jacob Alsterda ◽

Rohit R. Arora

Keyword(s):

Cholesteryl Ester ◽

Cholesteryl Ester Transfer Protein ◽

Plasma Cholesterol ◽

Genetic Research ◽

Plasma Lipoproteins ◽

Pharmacologic Therapy ◽

Atherosclerotic Cardiovascular Disease ◽

Current Standard ◽

Transfer Protein ◽

Cetp Inhibitors

The cholesteryl ester transfer protein (CETP) is a plasma protein that plays an important role in the transfer of lipids between plasma lipoproteins. The CETP inhibitors have been widely studied as a pharmacologic therapy to target plasma cholesterol in order to reduce the risk of atherosclerotic cardiovascular disease . Using CETP inhibitors as cholesterol modifiers was based on the genetic research that found correlations between CETP activity and cholesterol levels. Although CETP inhibitors are successful at altering targeted cholesterol markers, recent phase 3 outcome trials have shown limited benefit on cardiovascular outcomes when combined with the current standard of care. We discuss the science of CETP inhibition, compare the CETP inhibitors developed (torcetrapib, evacetrapib, dalcetrapib, and anacetrapib), the findings from the CETP inhibitor trials, and the future outlook for CETP inhibitors in cholesterol modification.

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