Target intelligence / Profile preview

Cyclooxygenase enzyme (official: Prostaglandin-endoperoxide synthase) (COX (or PTGS in genetics, but COX is dominant in medicine))

Target
COX (or PTGS in genetics, but COX is dominant in medicine)
Molecular classification
Enzyme, Heme peroxidase family member
01

Overview

Cyclooxygenase enzymes (COX, officially prostaglandin-endoperoxide synthase) are key mediators in the conversion of arachidonic acid into prostaglandins and thromboxanes, which regulate inflammation, pain, fever response, and platelet aggregation. COX-1 is constitutively expressed and maintains physiological functions such as gastric mucosal integrity and renal blood flow, whereas COX-2 is primarily inducible and mediates inflammatory responses. Both isoforms are targeted by NSAIDs, which provide anti-inflammatory and analgesic effects but can also lead to notable adverse effects such as gastrointestinal toxicity and increased cardiovascular risk. COX-2 is often overexpressed in cancers, making it a therapeutic and prognostic target

Other names
Prostaglandin-endoperoxide synthaseProstaglandin G/H synthasePGHSCOX-1COX-2PTGS1PTGS2
02

Mechanism of action

Nonselective COX inhibition (aspirin, ibuprofen, naproxen): blocks both COX-1 and COX-2 - Selective COX-2 inhibition (celecoxib, etoricoxib): blocks only COX-2 - Irreversible acetylation (aspirin): permanently inactivates COX

03

Biological functions

Prostaglandin biosynthesisThromboxane biosynthesisRegulation of inflammationPlatelet aggregation/clottingMaintenance of physiological homeostasis (gastrointestinal, renal, vascular functions)
04

Disease associations

InflammationPainFeverCancer (especially COX-2 overexpression)Cardiovascular disease (thrombotic risk)Neurodegenerative diseaseInfection
05

Safety considerations

Gastrointestinal toxicity (ulcer, bleeding) from COX-1 inhibitionCardiovascular risk (thrombosis, myocardial infarction) from COX-2 inhibitionRenal dysfunctionAllergic reactions due to leukotriene shunt
06

Interacting drugs

Aspirin

6 more in the full profile.

07

Biomarkers

COX-2 expression level (biomarker for cancer, inflammation, drug selection)Prostanoid levels (prostaglandins, thromboxane - for efficacy monitoring)

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