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

Bioorganicheskaia khimiia Pub Date : 2013-09-01

Jian Jing

引用次数: 0

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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新型抗血小板药物lys - gly - asp -环七肽的合成及活性研究。

首先合成线性七肽Cys-Lys-Gly-Asp-Trp-Asp-Cys，然后在Cys1和Cys7之间形成二硫键，形成含有lys - gly - asp -序列的环七肽。结构模拟表明，Lys-Gly-Asp-motif (KDG)具有功能性构象。该环七肽通过与血小板细胞膜上的GPIIb-IIIa受体特异性识别和相互作用，显示出强大的抗血小板聚集活性。其特异而有效的抗血小板活性使含kgd的环七肽成为一种可能的治疗剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Bioorganicheskaia khimiia

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