Stapling peptide and application thereof

By modifying the structure of the template peptide SLP-0 and replacing key amino acid residues with lysine, a staple peptide is formed, which solves the hemolytic problem, improves antibacterial activity and structural stability, and is suitable for the preparation of antibacterial drugs.

CN121005764APending Publication Date: 2025-11-25SHANDONG CENT FOR DISEASE CONTROL & PREVENTION +1
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Patent Information

Application Number
CN202510227850.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-08-05
Publication Date
2025-11-25

AI Technical Summary

Technical Problem

The existing template peptide SLP-0 has hemolytic problems during application, which limits its further development and application.

Method used

By modifying the structure of SLP-0 and replacing specific amino acid residues with lysine (Lys), staple peptides are formed, such as Ac-LKRVWKRVFKLLKS5YWRS5LKKPVR-NH2, in which amino acid residues 1L, 4V, 5W, 8V, 9F, 11L, 12L, 15Y, 16W, 19L, and 22P are replaced with Lys, forming structurally stable staple peptides.

Benefits of technology

The hemolytic activity of staple peptides was improved, significantly enhancing their antibacterial activity against Streptococcus pneumoniae, methicillin-resistant Staphylococcus aureus, Pseudomonas aeruginosa, and Klebsiella pneumoniae, demonstrating their potential as novel antibacterial drugs, while maintaining their resistance to proteolytic degradation.

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Abstract

The invention belongs to the field of polypeptide medicines, and particularly relates to stapled peptide and application thereof. According to the present invention, Ac-LKRVWKRVFKLLKS5YWRS5LKKPVR-NH2 is adopted as a peptide chain template, and an amino acid residue 15Y is replaced by K so as to obtain the target stapled peptide SLP-8; compared with the template polypeptide, the hemolytic activity of the obtained stapled peptide SLP-8 is obviously improved.
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