Cholesteryl Ester Transfer Protein (CETP) Inhibitors: Is There Life After Torcetrapib?

2008 ◽  
Vol 26 (4) ◽  
pp. 537-546 ◽  
Author(s):  
Hemanth Neeli ◽  
Daniel J. Rader
Keyword(s):  
Cholesteryl Ester ◽  
Cholesteryl Ester Transfer Protein ◽  
Transfer Protein ◽  
Cetp Inhibitors

Cholesteryl Ester Transfer Protein Inhibitors

2016 ◽  
Vol 22 (2) ◽  
pp. 99-104 ◽  
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.

scholarly journals Cholesteryl Ester Transfer Protein (CETP) Deficiency and CETP Inhibitors

2014 ◽  
Vol 37 (11) ◽  
pp. 777-784 ◽  
Author(s):  
Hiroshi Mabuchi ◽  
Atsushi Nohara ◽  
Akihiro Inazu
Keyword(s):  
Cholesteryl Ester ◽  
Cholesteryl Ester Transfer Protein ◽  
Transfer Protein ◽  
Cetp Inhibitors

QSAR study of a series of cholesteryl ester transfer protein inhibitors

2011 ◽  
Vol 76 (7) ◽  
pp. 803-813 ◽  
Author(s):  
Mahesh T. Chhabria ◽  
Bhanubhai N. Suhagia ◽  
Appaji B. Mandhare ◽  
Pathik S. Brahmkshatriya
Keyword(s):  
Cholesteryl Ester ◽  
Cholesteryl Ester Transfer Protein ◽  
Quantitative Structure Activity Relationship ◽  
Qsar Study ◽  
Transfer Protein ◽  
Cetp Inhibitors ◽  
Promising Target ◽  
Parabolic Relationship ◽  
Antihyperlipidemic Agents ◽  
Hdl Metabolism

Cholesteryl ester transfer protein (CETP), an enzyme which catalyses the transfer of cholesteryl ester from HDL to VLDL, is a promising target for discovery of novel antihyperlipidemic agents due to its pivotal role in HDL metabolism and reverse cholesterol transport. Quantitative structure activity relationship study of a series of CETP inhibitors was carried out using genetic function approximation to study various structural requirements for CETP inhibition. Various lipophilic, electronic, geometric and spatial descriptors were correlated with CETP inhibitory activity. Developed models were found predictive as indicated by their good r2pred values and satisfactory internal and external cross-validation results. Study reveals that lipophilicity (ClogP), with parabolic relationship, contributed significantly to the activity along with some electronic, geometric and quantum mechanical descriptors. The present study can be applied to future lead optimization of CETP inhibitors.

scholarly journals 52Therapy with cholesteryl ester transfer protein (CETP) inhibitors and diabetes risk. A Meta-analysis

2018 ◽  
Vol 39 (suppl_1) ◽  
Author(s):  
L M Lobo ◽  
W Masson ◽  
G Molinero ◽  
D Siniawski ◽  
M Huerin ◽  
...  
Keyword(s):  
Cholesteryl Ester ◽  
Cholesteryl Ester Transfer Protein ◽  
Meta Analysis ◽  
Diabetes Risk ◽  
Transfer Protein ◽  
Cetp Inhibitors

Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores

2021 ◽  
Vol 32 ◽  
pp. 127668
Author(s):  
Jian Liu ◽  
Patrick P. Shao ◽  
Deodial Guiadeen ◽  
Arto Krikorian ◽  
Wanying Sun ◽  
...  
Keyword(s):  
Cholesteryl Ester ◽  
Cholesteryl Ester Transfer Protein ◽  
Transfer Protein ◽  
Cetp Inhibitors
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