Lipidation of Naturally Occurring α-Helical Antimicrobial Peptides as a Promising Strategy for Drug Design.

ABSTRACT: In this paper, we describe the chemical synthesis, preliminary evaluation of antimicrobial properties and mechanisms of action of a novel group of lipidated derivatives of three naturally occurring α-helical antimicrobial peptides, LL-I (VNWKKVLGKIIKVAK-NH₂), LK6 (IKKILSKILLKKL-NH₂), ATRA-1 (KRFKKFFKKLK-NH₂). The obtained results showed that biological properties of the final compounds were defined both by the length of the fatty acid and by the structural and physico-chemical properties of the initial peptide. We consider C₈-C₁₂ length of the hydrocarbon chain as the optimal for antimicrobial activity improvement. However, the most active analogues exerted relatively high cytotoxicity toward keratinocytes, with the exception of the AT

SUBMITTER: Makowska M 

PROVIDER: S-EPMC9959048 | biostudies-literature | 2023 Feb

REPOSITORIES: biostudies-literature