Abstract
Polybia-MP1 is a well-known natural antimicrobial peptide isolated from the venom of the social wasp Polybia paulista. A recent study showed that this peptide displays a broad antibacterial spectrum as well as low toxicity to human red blood cells and normal fibroblasts. However, its moderate antimicrobial activity and high susceptibility to protease have been a major hurdle for clinical use. This study examined the possibility of developing biologically more potent, yet metabolically more stable, analogues of MP1 using an emerging technology termed “all-hydrocarbon stapling.” The stapled analogues of MP1 showed more than a threefold increase in helicity as well as an approximately 70-fold enhancement in proteolytic stability. These stapled analogues also exhibited a significant increase in inhibition against some Gram-positive bacteria while displaying a modest enhancement in hemolytic activity. Overall, the current study demonstrated that the all-hydrocarbon stapling system is a highly useful tool for the development of biologically more potent and metabolically more stable analogues of natural antimicrobial peptides.
Original language | English |
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Pages (from-to) | 1414-1419 |
Number of pages | 6 |
Journal | Archives of Pharmacal Research |
Volume | 40 |
Issue number | 12 |
DOIs | |
State | Published - 1 Dec 2017 |
Keywords
- Amphipathic peptides
- Antimicrobial peptides
- Proteolytic resistance
- Stapled peptides
- α-Helix