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Target intelligence / Profile preview
Prostacyclin synthase (PTGIS)
- Target
- PTGIS
- Molecular classification
- Enzyme, Cytochrome P450 superfamily
01
Overview
Prostacyclin synthase (PTGIS), also known as CYP8A1, is an enzyme that catalyzes the conversion of prostaglandin H2 (PGH2) to prostacyclin (PGI2). PGI2 is a potent vasodilator and inhibitor of platelet aggregation, playing a crucial role in maintaining vascular homeostasis. PTGIS is a member of the cytochrome P450 superfamily but functions as an isomerase rather than a monooxygenase. Its activity is critical in preventing thrombosis and cardiovascular diseases.
- Other names
- CYP8A1Prostaglandin-I synthase
02
Mechanism of action
Inhibition of PGH2 isomerization to PGI2 is a potential mechanism, but direct inhibitors are not widely used. Modulation of expression via gene transfer is also under investigation.
03
Biological functions
Catalysis of PGH2 to PGI2VasodilationInhibition of platelet aggregationEicosanoid metabolism
04
Disease associations
Cardiovascular diseaseMyocardial infarctionStrokeAtherosclerosisThrombosis
05
Safety considerations
Imbalance between prostacyclin and thromboxane A2Potential for off-target effects due to cytochrome P450 family membership
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