Target intelligence / Profile preview

Prostaglandin-endoperoxide synthase (commonly referred to as Cyclooxygenase) (COX)

Target
COX
Molecular classification
Enzyme, Oxidoreductase, Animal-type heme peroxidase family
01

Overview

Prostaglandin-endoperoxide synthases (commonly known as cyclooxygenases, COX) are key enzymes in the conversion of arachidonic acid to prostaglandins and thromboxanes, which mediate inflammation, pain, fever, and other physiological processes. There are two main isoforms: COX-1, constitutively expressed and maintaining normal physiological function such as gastric mucosa protection and platelet aggregation, and COX-2, predominantly induced in response to inflammatory stimuli and implicated in pathological conditions including inflammation and cancer. Pharmaceutical inhibition of COX enzymes by NSAIDs and selective COX-2 inhibitors is central in the management of inflammation, pain, and related disorders, though use is associated with notable safety risks such as gastrointestinal injury and cardiovascular events

Other names
CyclooxygenaseProstaglandin G/H synthasePTGSProstaglandin-endoperoxide synthaseProstaglandin synthaseProstaglandin-endoperoxide synthetasePHS
02

Mechanism of action

Reversible or irreversible inhibition of cyclooxygenase activity, blocking conversion of arachidonic acid to prostaglandins and thromboxane. (Aspirin acetylates the active site serine, producing irreversible inhibition, NSAIDs act reversibly, COX-2-selective inhibitors target the COX-2 isoenzyme selectively)

03

Biological functions

Prostanoid biosynthesis (prostaglandins, thromboxane)Inflammatory responsePain modulationPlatelet aggregationRegulation of renal and gastric function
04

Disease associations

InflammationPain disordersFeverThrombosis/cardiovascular diseaseCancer (esp. COX-2 in tumorigenesis)Neurodegenerative disease
05

Safety considerations

Gastrointestinal toxicity (e.g., ulcers, bleeding; more with nonselective inhibitors)Renal impairmentCardiovascular risk (especially with COX-2-selective inhibitors, e.g., myocardial infarction, stroke)Hypersensitivity and allergyPlatelet inhibition and bleeding risk (COX-1 inhibition)
06

Interacting drugs

Aspirin

7 more in the full profile.

07

Biomarkers

COX-2 expression in tumors (as a biomarker for cancer prognosis or to predict benefit from COX-2 inhibition)Prostaglandin E2 (PGE2) or thromboxane B2 (for activity monitoring)

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