Target intelligence / Profile preview

Phospholipase A2 group IVA (cPLA2α)

Target
cPLA2α
Molecular classification
Enzyme, Lipase, Cytosolic phospholipase A2 (cPLA2), Member of phospholipase A2 enzyme superfamily
01

Overview

Phospholipase A2 group IVA (cPLA2α) is a critical cytosolic enzyme responsible for hydrolyzing membrane phospholipids at the sn-2 position, which liberates arachidonic acid as a precursor for eicosanoid biosynthesis—including prostaglandins and leukotrienes that mediate cellular inflammatory responses and vascular homeostasis. Activation of cPLA2α is tightly regulated by intracellular calcium and phosphorylation, triggering its translocation from the cytosol to intracellular membranes (especially perinuclear membranes). Genetic variants of the PLA2G4A gene, encoding cPLA2α, are implicated in certain inherited bleeding disorders and may contribute to the pathophysiology of inflammatory, cardiovascular, and autoimmune diseases. The enzyme's pro-inflammatory role makes it an attractive—but challenging—therapeutic target for selective anti-inflammatory drug development.

Other names
Cytosolic phospholipase A2 alphacPLA2αPLA2G4A
02

Mechanism of action

Inhibition of cPLA2α blocks the release of arachidonic acid, thereby reducing the synthesis of downstream pro-inflammatory eicosanoids (prostaglandins, leukotrienes). Targeting cPLA2α affects inflammatory signal transduction and may diminish inflammatory and thrombotic responses.

03

Biological functions

Hydrolysis of membrane phospholipidsRelease of arachidonic acidBiosynthesis of eicosanoids (prostaglandins, leukotrienes)Regulation of inflammatory responsesSignal transductionGeneration of lysophospholipids involved in platelet-activating factor biosynthesis
04

Disease associations

InflammationAutoimmune disordersGastrointestinal ulceration with dysfunctional plateletsBleeding disorders (e.g., cytosolic phospholipase-A2 alpha deficiency associated bleeding disorder)Potential role in neurodegeneration and cardiovascular disease
05

Safety considerations

Inhibition may impair essential physiological functions such as hemostasis (blood clotting) because eicosanoids have diverse biological roles beyond inflammation.Potential risk for increased bleeding tendencies.Concerns about long-term suppression of eicosanoid signaling affecting cardiovascular and immune homeostasis
06

Interacting drugs

There are research-grade inhibitors of cPLA2α, but as of now, no widely used approved drugs directly target cPLA2α for clinical use.

1 more in the full profile.

07

Biomarkers

Increased cPLA2α activity levels or expression (often measured in tissues or plasma) can serve as a biomarker for inflammation and eicosanoid-mediated diseasesElevated levels of arachidonic acid or its metabolites can reflect cPLA2α activity

Beyond the preview

Go deeper on Phospholipase A2 group IVA (cPLA2α).

Explore the evidence, development activity, and competitive landscape with Gosset’s full data platform.

Drug pipeline

Full profile access

Explore the programs pursuing this target and their development progress.

  • Drug candidates
  • Developers
  • Development stage

Clinical trials

Full profile access

Follow the clinical studies evaluating therapies directed at this target.

  • Trial design
  • Status
  • Readouts

Competitive landscape

Full profile access

Compare approaches across drug candidates, modalities, and indications.

  • Programs
  • Modalities
  • Indications

Literature & evidence

Full profile access

Investigate the research and source evidence behind target biology and development.

  • Publications
  • Sources
  • Analysis

Patents

Full profile access

Explore patent activity around therapies and technologies addressing this target.

  • Patents
  • Assignees
  • Technologies

Research & analysis

Full profile access

Connect target biology, drug development, and emerging evidence in your research.

  • Biology
  • Development news
  • Analysis

Bring the full picture into focus.

See how Gosset can support your research on Phospholipase A2 group IVA (cPLA2α).

Explore the full profile

Gosset Free

Get started with Gosset.

Enter your work email and we’ll be in touch with next steps.

Work email preferred.

Book a call