PAR-1 Antagonist – GPCR Modulators

YFLLRNP works as a partial PAR-1 agonist that induces platelet shape change without calcium mobilization via the galpha12/13 signalling cascade. Full activation of platelets is only achieved at higher concentrations. YFLLRNP may therefore be useful for differentiating between several possible activation states of the platelet thrombin receptor. YFLLRNP is an antagonist to thrombin. 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.

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