Target intelligence / Profile preview

Prostaglandin-endoperoxide synthase (COX)

Target
COX
Molecular classification
Enzyme, Oxidoreductases (specifically heme peroxidases), Fatty acid oxygenases
01

Overview

Prostaglandin biosynthesis refers to the enzymatic process by which arachidonic acid is converted into various bioactive lipid mediators called prostaglandins. This process begins with the release of arachidonic acid from membrane phospholipids via phospholipase A₂. The key rate-limiting step is catalyzed by cyclooxygenases—prostaglandin-endoperoxide synthases—which convert arachidonic acid into unstable intermediates PGG₂ then PGH₂. Various terminal synthetic enzymes then generate distinct classes of biologically active prostaglandins including PGE₂, PGD₂, PGF₂α, PGI₂ (prostacyclin), and thromboxanes. These molecules regulate diverse physiological processes including inflammation, pain perception, vascular homeostasis, platelet function, gastrointestinal protection, renal function—and play roles in pathologies ranging from acute inflammation to chronic diseases like cancer and cardiovascular disorders.

Other names
CyclooxygenaseProstaglandin G/H synthaseProstaglandin-endoperoxide synthetaseCOX-1 / PTGS1COX-2 / PTGS2
02

Mechanism of action

Drugs targeting this pathway typically act by: - Inhibiting cyclooxygenases to block conversion of arachidonic acid into prostaglandins/thromboxanes. - Reducing synthesis of pro-inflammatory mediators.

03

Biological functions

Biosynthesis of eicosanoids/prostanoidsRegulation of inflammation and immune responseMediation of pain and fever responsesRegulation of vascular tone and platelet aggregation
04

Disease associations

InflammationPain disordersCardiovascular disease (thrombosis/atherosclerosis)Cancer progression in some contexts
05

Safety considerations

Gastrointestinal toxicity/ulceration from non-selective NSAIDs due to suppression of protective gastric mucosal PGsIncreased cardiovascular risk with selective COX-2 inhibitors due to imbalance between thromboxane A₂ and prostacyclin
06

Interacting drugs

Nonsteroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen, naproxen

2 more in the full profile.

07

Biomarkers

Urinary or plasma levels of specific prostaglandins/metabolites (for efficacy monitoring in research settings)

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