Macrocyclic hexapeptide analogues of the thrombin receptor (PAR-1) activation motif SFLLRN |
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| Authors: | McComsey D F Hecker L R Andrade-Gordon P Addo M F Maryanoff B E |
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| Institution: | R. W. Johnson Pharmaceutical Research Institute, Spring House, PA 19477, USA. |
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| Abstract: | The thrombin receptor (PAR-1) is activated by alpha-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 alpha-thrombin. Derivative 3c was the most potent macrocycle in activating PAR-1, with an EC50 of 24 microM. |
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