Target intelligence / Profile preview

Cyclooxygenase-1 (COX-1) (or, in certain contexts, Cyclooxygenase-2 (COX-2)) (COX-1 (also COX-2, when induced in inflammation))

Target
COX-1 (also COX-2, when induced in inflammation)
Molecular classification
Enzyme, Oxidoreductase, Lipid-metabolizing enzyme
01

Overview

Cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) are key enzymes responsible for the conversion of arachidonic acid to prostaglandins in the gastric mucosa; COX-1 is constitutively expressed and mediates baseline protective prostaglandin production, while COX-2 is inducible during inflammation. Prostaglandins synthesized in the gastric mucosa are essential for maintaining mucosal integrity, regulating acid secretion, and promoting epithelial cell restitution. Inhibition of COX enzymes, particularly by nonsteroidal anti-inflammatory drugs (NSAIDs), reduces mucosal prostaglandin synthesis and increases susceptibility to gastric injury and ulceration. Conversely, prostaglandin analogs such as misoprostol can supplement protective prostaglandins and are used clinically to prevent NSAID-induced ulcers.

Other names
Prostaglandin G/H synthaseCyclooxygenasePTGS1 (for COX-1)PTGS2 (for COX-2)
02

Mechanism of action

Inhibition of cyclooxygenase activity, reducing prostaglandin synthesis (nonselective and selective NSAIDs); Mimicry or supplementation of prostaglandins (e.g., misoprostol)

03

Biological functions

Prostaglandin synthesisGastric mucosal protectionInflammatory response modulationHomeostasis of gastric epithelial cells
04

Disease associations

Gastric ulcerationGastric mucosal injuryInflammationCancer (COX-2 especially)
05

Safety considerations

NSAID-induced gastric ulceration/bleeding (due to suppressed mucosal prostaglandin synthesis)Renal dysfunctionCardiovascular risks (especially with COX-2 selectives)Impaired gastric mucosal protection
06

Interacting drugs

Aspirin

8 more in the full profile.

07

Biomarkers

Gastric mucosal prostaglandin E2 levelsGastric mucosal prostaglandin F2alpha levelsCyclooxygenase expression (COX-1, COX-2 mRNA/protein levels)

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