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Updated: Jul 5, 2026

Protein Target Prediction and Validation of Small Molecule Compound

Protein Target Prediction and Validation of Small Molecule Compound

Published on: February 23, 2024

Viability of developing CETP inhibitors.

Cesare R Sirtori¹, Giuliana Mombelli

¹Department of Pharmacological Sciences, University of Milan, Milan, Italy. cesare.sirtori@unimi.it

Cardiovascular Therapeutics

|May 20, 2008

Summary

Cholesterol ester transfer protein (CETP) inhibition failed in trials, suggesting it is not a viable cardiovascular prevention target. CETP stimulation may offer a better approach for cardiovascular health.

Area of Science:

Cardiovascular disease
Pharmacology
Lipid metabolism

Background:

Cholesterol ester transfer protein (CETP) is a key regulator of lipoprotein metabolism.
Elevated high-density lipoprotein (HDL) cholesterol is a desirable therapeutic target for cardiovascular disease prevention.

Purpose of the Study:

To evaluate the viability of CETP inhibition as a therapeutic strategy for cardiovascular disease.
To explore alternative approaches for cardiovascular prevention targeting CETP.

Main Methods:

Review of existing literature on CETP inhibition.
Analysis of epidemiological data from individuals with CETP mutations.
In-depth analysis of pharmacological interventions targeting CETP.

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Last Updated: Jul 5, 2026

Protein Target Prediction and Validation of Small Molecule Compound

Protein Target Prediction and Validation of Small Molecule Compound

Published on: February 23, 2024

Main Results:

Major CETP inhibitors have failed in clinical trials for high-risk coronary patients.
The rationale for CETP inhibition appears weak, with limited benefits for cardiovascular prevention.
Clinical studies showed a significant increase in infectious complications with CETP inhibitors.

Conclusions:

CETP inhibitory treatment should not be pursued as a viable approach for cardiovascular prevention.
CETP stimulation, potentially via compounds like probucol, may offer a more promising strategy for cardiovascular health.