De Novo Design and Their Antimicrobial Activity of Stapled Amphipathic Helices of Heptapeptides

Bulletin of the Korean chemical society

Thuy T. T. Dinh¹  Young-Woo Kim¹  Do-Hee Kim¹  Bong-Jin Lee¹ 

关键词: Antimicrobial peptides;    -Helix;    Stapled peptides;    Protease resistance;    Peptide drugs;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

In this study we designed and synthesized several heptapeptides that are enforced to form an amphipathic helix using all-hydrocarbon stapling system and evaluated their antimicrobial and hemolytic activities. The antimicrobial activity showed clear structure-activity relationships, confirming the importance of helicity and amphipathicity. Some stapled heptapeptides displayed a moderate antimicrobial activity along with a low hemolytic activity. To our best knowledge, although not highly potent, these stapled peptides represent the shortest helical amphipathic antimicrobial peptides reported to date. The preliminary data obtained in this work would serve as a good starting point for further developing short analogs of amphipathic helical antimicrobial peptides.

【 授权许可】

Unknown