Target intelligence / Profile preview

Cyclooxygenase-2 and Heme oxygenase-1 (COX-2 and HO-1)

Target
COX-2 and HO-1
Molecular classification
Enzyme
01

Overview

Cyclooxygenase-2 (COX-2), also known as Prostaglandin-endoperoxide synthase 2 (PTGS2), is an inducible enzyme that catalyzes the conversion of arachidonic acid to prostaglandins, which are key mediators of inflammation and pain (UniProt P35354). Heme oxygenase-1 (HO-1), or HMOX1, is the rate-limiting enzyme in heme degradation, producing biliverdin, carbon monoxide, and iron, which collectively exert antioxidant and anti-inflammatory effects (UniProt P09601). These two proteins are often studied in tandem because many anti-inflammatory agents work by simultaneously inhibiting COX-2 and inducing HO-1 expression, often through the Nrf2 signaling pathway (PubMed: 25634308). While COX-2 inhibition reduces pro-inflammatory mediators, HO-1 induction enhances cellular defenses against oxidative stress and further suppresses inflammatory cytokines. This dual modulation is a common pharmacological strategy in treating inflammatory diseases and certain cancers. However, 'COX-2 and HO-1 expression' refers to a combined biological readout or a dual-target approach rather than a single molecular target entity.

Other names
PTGS2 and HMOX1Prostaglandin-endoperoxide synthase 2 and Heme oxygenase 1COX-2/HO-1 axis
02

Mechanism of action

Inhibition of COX-2 enzymatic activity and transcriptional induction of HO-1 expression.

03

Biological functions

InflammationOxidative stress responseCytoprotectionHeme catabolismProstaglandin biosynthesis
04

Disease associations

InflammationCancerCardiovascular diseaseNeurodegenerative disease
05

Safety considerations

Cardiovascular events (COX-2 inhibitors)Gastrointestinal toxicityPotential for HO-1 to promote tumor progression in established cancers
06

Interacting drugs

Celecoxib

5 more in the full profile.

07

Biomarkers

Prostaglandin E2 (PGE2)BilirubinCarbon monoxideCOX-2 protein levelsHO-1 protein levels

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