Related Experiment Video

Updated: May 20, 2026

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2
10:31

A Liposome Membrane Permeability Assay for Investigating the Effects of Phosphatidylinositol Phosphate Groups on Membranotropic Action of Venom PLA2

Published on: September 26, 2025

Phospholipase A2 enzymes and the risk of atherosclerosis

Robert S Rosenson1, Eva Hurt-Camejo

  • 1Mount Sinai School of Medicine, 1425 Madison Ave., Box 1030, New York, NY 10029, USA. robert.rosenson@mssm.edu

European Heart Journal
|July 18, 2012
PubMed

Insights

Certain phospholipase A(2) enzymes are linked to atherosclerosis. Inhibiting secretory phospholipase A(2) (sPLA(2)) and lipoprotein-associated phospholipase A(2) (Lp-PLA(2)) shows promise for preventing cardiovascular events.

Area of Science:

  • Biochemistry
  • Cardiovascular Medicine
  • Enzymology

Background:

  • The phospholipase A(2) enzyme superfamily is implicated in the pathogenesis of atherosclerosis.
  • Specific members, secretory phospholipase A(2) (sPLA(2)) and lipoprotein-associated phospholipase A(2) (Lp-PLA(2)), are key targets for cardiovascular disease prevention.

Purpose of the Study:

  • To review the experimental and human evidence supporting the development of inhibitors for sPLA(2) and Lp-PLA(2) in cardiovascular outcome trials.
  • To assess the potential of these enzyme inhibitors for preventing cardiovascular events.

Main Methods:

  • Review of experimental animal studies, human biomarker data, vascular imaging, and genome-wide association studies.
  • Analysis of ongoing and recently terminated clinical trials for sPLA(2) and Lp-PLA(2) inhibitors.

Main Results:

  • Clinical trials involving sPLA(2) inhibitors (e.g., varespladib methyl) have been conducted, with some terminated.
  • Clinical trials for Lp-PLA(2) inhibitors (e.g., darapladib) are ongoing in patients with coronary heart disease.

Conclusions:

  • Inhibition of sPLA(2) and Lp-PLA(2) represents a rational therapeutic strategy for cardiovascular event prevention.
  • Further clinical evaluation is necessary to establish the efficacy and safety of these enzyme inhibitors.

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