221301-45-7Relevant academic research and scientific papers
Macrocyclic hexapeptide analogues of the thrombin receptor (PAR-1) activation motif SFLLRN
McComsey, David F.,Hecker, Leonard R.,Andrade-Gordon, Patricia,Addo, Michael F.,Maryanoff, Bruce E.
, p. 255 - 260 (1999)
The thrombin receptor (PAR-1) is activated by α-thrombin to stimulate various cell types, including platelets, through the tethered-ligand sequence SFLLRN. Macrocyclic peptide analogues of SFLLRN were synthesized and evaluated in vitro. In general, the compounds were much less potent in inducing platelet aggregation relative to SFLLRN-NH2 and did not act as antagonists of α-thrombin. Derivative 3c was the most potent macrocycle in activating PAR-1, with an EC50 of 24 μM.
