Antimicrobial and Hemolytic Activity of Stapled Heptapeptide Dimers

Bulletin of the Korean Chemical Society

Do‐¹  Bong‐²  Young‐²  Woo Kim³  Huy X. Luong³  Jin Lee⁴  Hee Kim⁴ 

[1] 715 Korea;742 Korea;College of Pharmacy Dongguk University Seoul 100‐College of Pharmacy Seoul National University Seoul 151‐

关键词: Antimicrobial peptides;    α;    ‐;    Helix;    Stapled peptides;    Amphipathic helices;    Hemolytic activity;   

DOI  :  10.1002/bkcs.10839

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

To improve the antimicrobial activity of the hydrocarbon‐stapled amphipathic heptapeptide helix identified from our previous study, we prepared a series of its dimeric analogs using several different linkers. All of these dimers showed a significant increase in antimicrobial activity although their hemolytic activity was also largely increased. One particular analog bearing a proline linker displayed notably low hemolytic activity compared to others, indicating that the conformational characteristics of the linker play a key role in disassociating undesirable hemolytic activity from antimicrobial activity in this series of antimicrobial peptides. We believe that this analog can serve as a stepping stone for further development of novel antimicrobial agents to combat antibiotic‐resistance.

【 授权许可】

Unknown