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

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 im...

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Bibliographic Details
Published inBulletin of the Korean Chemical Society Vol. 35; no. 12; pp. 3632 - 3636
Main Authors Dinh, Thuy T.T, Kim, Do-Hee, Lee, Bong-Jin, Kim, Young-Woo
Format Journal Article
LanguageKorean
Published 2014
Subjects
Antimicrobial peptides
{\alpha}$-Helix
Peptide drugs
Protease resistance
Stapled peptides
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Summary: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.
Bibliography:KISTI1.1003/JNL.JAKO201436438765344
ISSN:0253-2964
1229-5949