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Cholesterol Efflux Assay
07:54

Cholesterol Efflux Assay

Published on: March 6, 2012

Cholesteryl ester transfer protein (CETP) inhibitors

Julianne A Hunt1, Zhijian Lu

  • 1Merck Research Laboratories, Rahway, NJ 07065, USA. julianne_hunt@merck.com

Current Topics in Medicinal Chemistry
|June 13, 2009
PubMed

Insights

Inhibiting cholesteryl ester transfer protein (CETP) increases high-density lipoprotein cholesterol (HDL-C). While this boosts HDL-C levels, its impact on reducing coronary heart disease (CHD) requires further investigation.

Area of Science:

  • Cardiovascular Medicine
  • Lipid Metabolism
  • Pharmacology

Background:

  • Epidemiological studies show lower high-density lipoprotein cholesterol (HDL-C) correlates with higher coronary heart disease (CHD) incidence.
  • Cholesteryl ester transfer protein (CETP) facilitates lipid transfer from HDL to apoB lipoproteins.
  • Targeting CETP is a strategy to elevate HDL-C levels.

Purpose of the Study:

  • To review the role of CETP in lipid metabolism.
  • To discuss recent advancements in small-molecule CETP inhibitors.
  • To explore the future potential of CETP inhibitors for CHD treatment.

Main Methods:

  • Review of epidemiological data on HDL-C and CHD.
  • Analysis of CETP function in lipid transfer.
  • Examination of pharmacological CETP inhibition studies in humans.

Main Results:

  • CETP inhibition demonstrably increases plasma HDL-C concentrations.
  • Pharmacological inhibition of CETP in humans leads to elevated HDL-C levels.
  • The clinical benefit of CETP inhibition on reducing CHD incidence remains to be established.

Conclusions:

  • CETP plays a complex role in regulating lipid profiles.
  • Small-molecule inhibitors offer a promising avenue for modulating CETP activity.
  • Further research is needed to confirm the efficacy of CETP inhibitors in preventing cardiovascular events.

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