PAR-2 Agonist amide – GPCR Modulators

Thrombin receptor inhibitory peptide (TRIP). Thrombin activates members of the PAR family of receptors to initiate a variety of signalling pathways. 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. This peptide mimics the tethered peptide ligand of PAR- 2, but lacks the S42 residue which is important for receptor activation, and therefore acts as a thrombin antagonist peptide.