Target intelligence / Profile preview

Prostaglandin I2 synthase (PTGIS)

Target
PTGIS
Molecular classification
Enzyme, Cytochrome P450 isomerase family
01

Overview

Prostaglandin I2 synthase (PTGIS), also known as prostacyclin synthase or CYP8A1, is an enzyme in the cytochrome P450 superfamily that catalyzes the conversion of prostaglandin H2 into prostacyclin (prostaglandin I2). Prostacyclin acts as a potent vasodilator and inhibitor of platelet aggregation. The balance between its production and that of thromboxane A2 plays a critical role in cardiovascular health. Dysregulation can contribute to conditions such as myocardial infarction and stroke. PTGIS is considered an important therapeutic target for cardiovascular diseases and pulmonary arterial hypertension; several drugs act by mimicking or enhancing its product's effects.[4][5][3]

Other names
prostacyclin synthaseprostaglandin-I synthasePGI2 synthaseCYP8A1PGISprostacyclin synthetaseprostagladin I2 synthetase
02

Mechanism of action

Agonism at the IP receptor leading to vasodilation and inhibition of platelet aggregation

03

Biological functions

Catalyzes conversion of prostaglandin H2 to prostacyclin (PGI2)VasodilationInhibition of platelet aggregation
04

Disease associations

Cardiovascular disease (e.g., myocardial infarction, stroke, atherosclerosis)Pulmonary arterial hypertensionInflammation and rheumatological diseases (e.g., rheumatoid arthritis)
05

Safety considerations

Bleeding risk due to inhibition of platelet aggregation
06

Interacting drugs

Epoprostenol (Flolan)

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