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Target intelligence / Profile preview
Protease-activated receptor 2 (PAR2)
- Target
- PAR2
- Molecular classification
- G protein-coupled receptor, GPCR, Protease-activated receptor, Class A GPCR
01
Overview
Protease activated receptor 2 (PAR2) is a widely expressed class-A GPCR that acts as a sensor for endogenous/exogenous serine proteases. It plays critical roles across inflammation/immunity/homeostasis/cancer/metabolism by integrating signals from its unique irreversible mode of activation. Its complex regulation involves both classical G protein-dependent pathways and β-arrestin scaffolding functions.
- Other names
- Coagulation factor II (thrombin) receptor-like 1G-protein coupled receptor 11F2RL1
02
Mechanism of action
Agonist binding, proteolytic cleavage exposing tethered ligand, G protein activation, β-arrestin recruitment
03
Biological functions
Signal transductionRegulation of epithelial barrier functionRegulation of epithelial differentiationAngiogenesisImmune cell recruitmentImmune cell activationModulation of metabolic pathwaysRegulation of vascular toneRegulation of blood flowEndothelial nitric oxide production
04
Disease associations
InflammationNeurogenic inflammationHyperalgesiaPain perceptionObesityCancerAsthmaLung injuryInflammatory bowel diseaseIrritable bowel syndromeVascular diseases
05
Safety considerations
Complex signaling pathways involving both G proteins and β-arrestinsPotential for off-target effects due to broad expressionDesensitization and downregulation mechanisms
06
Interacting drugs
Agonists (synthetic peptides mimicking tethered ligand)
1 more in the full profile.
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