Antimicrobial and hemolytic activity of stapled heptapeptide dimers

Huy X. Luong, Do Hee Kim, Bong Jin Lee, Young Woo Kim

Research output: Contribution to journalArticlepeer-review

19 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)1199-1203
Number of pages5
JournalBulletin of the Korean Chemical Society
Volume37
Issue number8
DOIs
StatePublished - 1 Aug 2016

Keywords

  • Amphipathic helices
  • Antimicrobial peptides
  • Hemolytic activity
  • Stapled peptides
  • α-helix

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