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- Title
Antimicrobial and Hemolytic Activity of Stapled Heptapeptide Dimers.
- Authors
Luong, Huy X.; Kim, Do-Hee; Lee, Bong-Jin; Kim, Young-Woo
- 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.
- Subjects
ANTI-infective agents; DIMERS; PEPTIDE antibiotics; PEPTIDES; AMPHIPHILES
- Publication
Bulletin of the Korean Chemical Society, 2016, Vol 37, Issue 8, p1199
- ISSN
0253-2964
- Publication type
Article
- DOI
10.1002/bkcs.10839