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Target intelligence / Profile preview
Cholesteryl Ester Transfer Protein (CETP)
- Target
- CETP
- Molecular classification
- Lipid Transfer Protein, Glycoprotein
01
Overview
Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that mediates the transfer of cholesteryl esters and triglycerides between lipoproteins, primarily between HDL and LDL/VLDL. Inhibiting CETP is a therapeutic strategy aimed at raising HDL-C and lowering LDL-C to reduce the risk of cardiovascular disease. CETP is synthesized in the liver and has a boomerang-shaped structure with a central tunnel for lipid transport. Its activity influences cholesterol homeostasis and the distribution of cholesterol among lipoproteins.
- Other names
- Plasma lipid transfer protein
02
Mechanism of action
CETP inhibitors reduce CETP activity, leading to increased HDL-cholesterol and decreased LDL-cholesterol levels by inhibiting the transfer of cholesteryl esters from HDL to LDL/VLDL.
03
Biological functions
Lipid transportCholesterol homeostasisReverse cholesterol transportTriglyceride metabolism
04
Disease associations
Cardiovascular diseaseAtherosclerosisDyslipidemiaMetabolic syndromeDiabetes mellitus
05
Safety considerations
Increased blood pressure (observed with some CETP inhibitors)Off-target effectsCardiovascular events (observed in some clinical trials)
06
Interacting drugs
Small molecule CETP inhibitors (e.g., torcetrapib, dalcetrapib, anacetrapib, evacetrapib)
3 more in the full profile.
07
Biomarkers
HDL-C levelsLDL-C levelsTriglyceride levelsCETP activity
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