De Novo design and their antimicrobial activity of stapled amphipathic helices of heptapeptides

Thuy T.T. Dinh, Do Hee Kim, Bong Jin Lee, Young Woo Kim

Research output: Contribution to journalArticlepeer-review

23 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)3632-3636
Number of pages5
JournalBulletin of the Korean Chemical Society
Volume35
Issue number12
DOIs
StatePublished - 20 Dec 2014

Keywords

  • Antimicrobial peptides
  • Peptide drugs
  • Protease resistance
  • Stapled peptides
  • α-Helix

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