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Target intelligence / Profile preview
Protease Activated Receptor 1 (PAR1)
- Target
- PAR1
- Molecular classification
- G protein-coupled receptor, Protease Activated Receptor
01
Overview
Protease activated receptor 1 (PAR1), also known as F2R, is a member of the protease-activated receptor family, which are G protein-coupled receptors (GPCRs). PAR1 was first identified in 1991 and is best known as the primary thrombin receptor on human platelets and endothelial cells. The unique activation mechanism involves proteolytic cleavage of its N-terminal ectodomain by specific proteases, exposing a new N-terminus that acts as a tethered ligand to activate the receptor. PAR1 is expressed widely in blood cells (including platelets), endothelial cells, epithelial cells, neurons and astrocytes, and immune cells. PAR1 plays roles in hemostasis/thrombosis; vascular integrity regulation; inflammation modulation; and cancer progression.
- Other names
- F2RThrombin receptor
02
Mechanism of action
Receptor antagonism; Allosteric inhibition
03
Biological functions
HemostasisThrombosisVascular integrity regulationInflammation modulationCell proliferationAngiogenesisSignal transduction
04
Disease associations
Cardiovascular diseaseInflammationCancerThrombotic disorders
05
Safety considerations
Bleeding risk (antiplatelet therapies)Potential for off-target effects due to widespread expression
06
Interacting drugs
Vorapaxar
2 more in the full profile.
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