Synthesis and activity of a cyclo-heptapeptide containing Lys-Gly-Asp-sequence as a novel anti-platelet agent.
Jing. Jian J
Key Findings
- A linear heptapeptide was cyclized via a disulfide bridge to create a stable cyclic peptide.
- The KGD motif in the cyclic structure adopts a shape that can interact with the GPIIb/IIIa receptor on platelets.
- The cyclic peptide showed potent anti‑platelet aggregation activity in vitro.
Practical Outcomes
- At this point the peptide is not something you can buy or use; it’s an early‑stage research compound. It suggests that KGD‑based cyclic peptides could become future anti‑clot agents, but more development and safety testing are needed before any real‑world protocols can be designed.
Summary
Researchers made a small circular protein that includes a Lys‑Gly‑Asp (KGD) piece and found it can strongly stop platelets from clumping together by attaching to a specific platelet receptor. The work is still at the lab‑test stage, with no human data or dosing information yet.
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.
Study Information
pubmed
2013