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Synthesis and activity of a cyclo-heptapeptide containing Lys-Gly-Asp-sequence as a novel anti-platelet agent

Abstract

Linear hepta-peptide Cys-Lys-Gly-Asp-Trp-Asp-Cys was synthesized first and then disulfide bond was formed between the Cys1 and Cys7 to develop cyclo-heptapeptide containing Lys-Gly-Asp-sequence. Structural simulation showed that Lys-Gly-Asp-motif (KDG) displayed functional conformation. The cyclo-heptapeptide exhibited potent anti-platelet aggregation activity based on specific recognition and interaction with the GPIIb-IIIa receptor on platelet cell membrane. The specific and potent anti-platelet activity makes the KGD-containing cyclo-heptapeptide a possible therapeutic agent.

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Correspondence to Jian Jing.

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Jing, J. Synthesis and activity of a cyclo-heptapeptide containing Lys-Gly-Asp-sequence as a novel anti-platelet agent. Russ J Bioorg Chem 39, 488–492 (2013). https://doi.org/10.1134/S1068162013050063

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  • DOI: https://doi.org/10.1134/S1068162013050063

Keywords

  • KGD-containing cyclo-heptapeptide
  • platelet aggregation inhibitory activity
  • integrin binding selectivity