Target intelligence / Profile preview

Cyclooxygenase enzyme (COX)

Target
COX
Molecular classification
Enzyme, Specifically, oxidoreductases (EC 1.14.99.1), Heme peroxidases
01

Overview

The *cyclooxygenases* (**COXs**) are key enzymes responsible for converting arachidonic acid into prostanoids—including prostaglandins and thromboxanes—which mediate inflammation, pain sensation, fever response, platelet aggregation/clotting processes, gastric mucosal protection, kidney function regulation, among other physiological roles.[3][6] There are two main isoforms in humans—COX‑1 (*prostaglandin-endoperoxide synthase 1*, PTGS1), which is constitutively expressed in most tissues for homeostatic functions; and COX‑2 (*prostaglandin-endoperoxide synthase 2*, PTGS2), which is inducible at sites of inflammation.[6][7] Pharmaceutical inhibitors targeting these enzymes—most notably NSAIDs—are widely used for their anti-inflammatory analgesic effects but carry risks related to gastrointestinal integrity (mainly via COX‑1) as well as cardiovascular safety concerns when selectively inhibiting only COX‑2.[8]

Other names
Prostaglandin-endoperoxide synthaseProstaglandin G/H synthasePTGS (gene/protein family)COX enzyme
02

Mechanism of action

Drugs targeting cyclooxygenases act by: - Reversibly or irreversibly inhibiting the enzymatic activity of COX‑1 and/or COX‑2. - Blocking conversion of arachidonic acid to prostaglandins and thromboxanes. - Reducing synthesis of mediators involved in inflammation, pain, fever, and platelet aggregation.

03

Biological functions

Biosynthesis of prostanoids (prostaglandins, thromboxane, prostacyclin)Regulation of inflammationPlatelet aggregation and blood clottingModulation of pain and fever responses
04

Disease associations

InflammationPain syndromesCardiovascular disease/thrombosisCancer/oncologyNeurodegenerative diseases
05

Safety considerations

Gastrointestinal ulceration/bleeding (especially with non-selective NSAIDs due to COX‑1 inhibition)Increased cardiovascular risk events such as heart attack/stroke with some selective COX‑2 inhibitorsRenal impairment/kidney injury due to altered renal blood flow regulation
06

Interacting drugs

Aspirin

6 more in the full profile.

07

Biomarkers

There are no widely used direct biomarkers for patient selection based on cyclooxygenase activity; however:Urinary or plasma levels of prostaglandin metabolites may reflect pathway activity in research settings.Platelet function tests can be used to monitor aspirin effect.

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