PAR-3 Agonist (Human) - GPCR Modulators

Protease activated receptors (PARs) are a distinctive four-member family of seven transmembrane G protein-coupled receptors (GPCRs) widely expressed in inflammatory cells. PARs are cleaved by certain serine proteases to expose a tethered ligand domain, this ligand domain then binds to and activates the receptors to initiate multiple signalling cascades. These PAR-activating proteases therefore represent PAR agonists. This PAR-3 agonist peptide represents the sequence of the 'tethered ligand' and is therefore capable of activating the receptor independently of N-terminal proteolysis. PAR-3 is required for intercellular adhesion molecule 1 (ICAM-1) expression in endothelial cells and PAR-3 cooperates with PAR-1 to mediate the effect of thrombin on cytokine production and vascular cell adhesion molecule (VCAM- 1) expression.