thrombin receptor peptide ligand

Thrombin receptor peptide ligand, a thrombin receptor antagonist, serves as an antithrombotic agent [1].

Thrombin receptor peptide ligand is antagonist of the thrombin receptor (EC50s = 16-33 μM to inhibit platelet aggregation in vitro). It inhibits α-thrombin and platelet aggregation induced by thrombin receptor activating peptide in vitro when used at a concentration of 32 μM but does not affect platelet aggregation induced by ADP or collagen. It also inhibits thrombin- and TRAP-induced proliferation of vascular smooth muscle cells (VSMCs). Thrombin receptor peptide ligand (100 μmol/kg bolus, i.v., plus 900 μmol/kg infusion) inhibits arterial thrombosis in a rabbit model of partial carotid artery occlusion without increasing bleeding time.

Protease-Activated Receptor-1, PAR-1 Agonist acetate is a selective proteinase-activated receptor1 (PAR-1) agonist peptide. Protease-Activated Receptor-1, PAR-1 Agonist acetate corresponds to PAR1 tethered ligand and which can selectively mimic theactions of thrombin via this receptor[1][2].

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].

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

Protease-Activated Receptor-1 (PAR-1) Agonist, a selective peptide, activates the PAR-1 receptor by mimicking the specific actions of thrombin. It corresponds to the PAR1 tethered ligand, facilitating selective activation of this receptor.

TFLLRNPNDK-NH2 is a biologically active peptide and a thrombin receptor activating peptide (TRAP). As a PAR-1 agonist, it reversibly binds to PAR-1, mimicking the 'tethered ligand' created by thrombin through proteolytic substrate cleavage. It also induces increased liquid and protein permeability, similar to thrombin's effect.

Ser-parafluoroPhe-Aad-Leu-Arg-Asn-Pro-NH2 is a biologically active peptide. Structure-activity studies of the thrombin receptor-tethered ligand SFLLRNP highlighted the pivotal role of the Phe-2-phenyl group in receptor recognition, while substitution with para-fluorophenylalanine [(p-F)Phe] increased its activity.