Bulletin of the Korean Chemical Society | |
Antimicrobial and Hemolytic Activity of Stapled Heptapeptide Dimers | |
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 hydrocarbonâstapled 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 antibioticâresistance.
【 授权许可】
Unknown
【 预 览 】
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