SYNTHESIS AND ACTIVITY OF A CYCLO-HEPTAPEPTIDE CONTAINING LYS-GLY-ASP-SEQUENCE AS A NOVEL ANTI-PLATELET AGENT
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Department of Bioorganic and Biological Chemistry, Beijing Key Lab, Beijng Normal University, Beijing, 100875, China
Received March 20, 2013; in final form, April 12, 2013
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.
Keywords: KGD-containing cyclo-heptapeptide, platelet aggregation inhibitory activity, integrin binding selectivity.
Биоорг.химия 2013, 39 (5): 547-551