Bioorganic and Medicinal Chemistry Letters p. 255 - 260 (1999)
Update date:2022-09-26
Topics:
McComsey, David F.
Hecker, Leonard R.
Andrade-Gordon, Patricia
Addo, Michael F.
Maryanoff, Bruce E.
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.
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