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Target intelligence / Profile preview
Protease-Activated Receptors (PARs)
- Target
- PARs
- Molecular classification
- G protein-coupled receptor, Receptor
01
Overview
Protease-activated receptors (PARs) are a unique subfamily of G protein-coupled receptors (GPCRs) that are activated by proteolytic cleavage of their extracellular N-terminal domain by serine proteases. This cleavage exposes a tethered ligand that binds intramolecularly, triggering conformational changes and activating intracellular signaling pathways. PARs mediate diverse physiological processes including hemostasis, inflammation, vascular biology, and gastrointestinal physiology. Dysregulation of PAR signaling contributes to several diseases, including thrombosis, cardiovascular diseases, cancer progression, and inflammatory disorders. PAR antagonists are under development as therapeutic agents.
- Other names
- PAR1PAR2PAR3PAR4
02
Mechanism of action
Antagonism of PAR subtypes, inhibition of protease-mediated activation
03
Biological functions
Signal transductionHemostasisInflammationVascular biologyGastrointestinal physiologyCardiovascular homeostasis
04
Disease associations
ThrombosisCardiovascular diseasesCoronary artery diseaseCancer progressionInflammatory disordersSARS-CoV‑2 infection
05
Safety considerations
Species differences between human and animal modelsPotential for off-target effects due to broad tissue distributionIrreversible activation mechanism poses challenges for drug development
06
Interacting drugs
PAR antagonists
2 more in the full profile.
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