期刊
CHEMISTRY-A EUROPEAN JOURNAL
卷 22, 期 24, 页码 8358-8367出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201600445
关键词
amino acids; antibiotics; membrane proteins; peptidomimetics; silicon
资金
- Danish National Research Foundation [DNRF59]
- Lundbeck Foundation
- Carlsberg Foundation
- Aarhus University
Incorporation of silicon-containing amino acids in peptides is known to endow the peptide with desirable properties such as improved proteolytic stability and increased lipophilicity. In the presented study, we demonstrate that incorporation of beta-silicon-beta 3-amino acids into the antimicrobial peptide alamethicin provides the peptide with improved membrane permeabilizing properties. A robust synthetic procedure for the construction of beta-silicon-beta 3-amino acids was developed and the amino acid analogues were incorporated into alamethicin at different positions of the hydrophobic face of the amphipathic helix by using SPPS. The incorporation was shown to provide up to 20-fold increase in calcein release as compared with wild-type alamethicin.
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