title: 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.
authors.affiliation: Department of Bioorganic and Biological Chemistry, Beijing Key Lab, Beijing Normal University, Beijing 100875, PR China.
authors.forename: Jian
authors.initials: J
authors.lastname: Jing
mesh_terms: D000595:Amino Acid Sequence; D006801:Humans; D009842:Oligopeptides / Q000008:administration & dosage / Q000138:chemical synthesis*; D010455:Peptides / Q000008:administration & dosage / Q000138:chemical synthesis*; D010974:Platelet Aggregation / Q000187:drug effects*; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D013329:Structure-Activity Relationship
chemical_list: D009842:Oligopeptides; D010455:Peptides; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; C533570:lysyl-glutamyl-aspartic acid