PAR-4 Agonist (Mouse) – GPCR Modulators

Thrombin is the main effector of the coagulation cascade- it is a serine protease. Thrombin binds to active protease activated receptor (PAR) which belongs to a subfamily of G-protein coupled receptors (GPCR). Thrombin activation of mouse PAR-4 reveals an amino terminus sequence of GYPGKF. This is the natural ligand for PAR-4. GYPGKF binds internally to the receptor and leads to signalling activation. Identification of GYPGKF as a PAR-4 agonist has allowed better understand of the function of PAR. Addition of GYPGKF to PAR-4 expressing cell lines achieved 55% of the maximal response of thrombin. GYPGKF can provide understanding of PAR-4 and a template for more potent agonists.