Protease-Activated Receptor-1 (PAR-1) Agonist TFA is a selective peptide that acts as an agonist for the proteinase-activated receptor-1 (PAR-1). Corresponding to the tethered ligand of PAR-1, this compound mimics the actions of thrombin through the PAR-1 receptor[1][2].

A Protease-Activated Receptor-1 (PAR-1) agonist triggers the activation of protein kinase C (PKC) isoforms alpha and epsilon in HT-29 colon carcinoma cells that endogenously express PAR1. This stimulation at the cellular level, induced by both the PAR-1 agonist and thrombin, leads to enhanced HT-29 cell migration and matrix adhesion through a PKCepsilon-dependent pathway. This conclusion is supported by the observation that the effects mediated by PAR1 are inhibited by bisindolylmaleimide I (a PKC inhibitor) and EAVSLKPT (a PKCepsilon translocation inhibitory peptide), but not by PKC inhibitor G? 6976[2].