PMID: 16637284Apr 28, 2006Paper

The structure-antiaggregative activity relationship in a series of Arg-Gly-Asp analogs

Bioorganicheskaia khimiia
O V Mel'nikV P Golubovich

Abstract

A series of analogues of Arg-Gly-Asp tripeptide, the common structural element of most of the integrin receptor ligands, possessing different conformational features for the interaction with platelet receptors, were synthesized by the methods of conventional peptide chemistry for use in the search for antithrombotic agents. The distance between the guanidine group of Arg and the beta-carboxyl group of Asp was shown to affect the antiaggregative activity. A potent inhibitor of platelet aggregation, tripeptide Arg-betaAla-Asp, with IC50 = 10.6 microM (ADP, 1.5 microM), was revealed.

References

Dec 1, 1985·Proceedings of the National Academy of Sciences of the United States of America·E F PlowM H Ginsberg
Oct 1, 1984·Proceedings of the National Academy of Sciences of the United States of America·M D Pierschbacher, E Ruoslahti
Jun 1, 1982·Proceedings of the National Academy of Sciences of the United States of America·E F Plow, G Marguerie

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Citations

Apr 22, 2015·Bioorganicheskaia khimiia·A Iu VigorovV P Krasnov
Feb 10, 2007·Bioorganic & Medicinal Chemistry Letters·Luca GentilucciMonica Baiula
Feb 16, 2008·Meditsinskaia tekhnika·O V Mel'nik

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