Tuning the Activity of Anoplin by Dendrimerization of Lysine and Lipidation of the N-Terminal.
2021
Dendrimeric antimicrobial peptides or lipopeptides have strong transmembrane ability and antibacterial activity. To obtain some ideal antimicrobial peptides, anoplin, a natural antimicrobial peptide with weak antimicrobial activity, was modified by C-terminal dendrimerization using lysine and N-terminal lipidation using fatty acids. 2K-3A-C4, a trimer of anoplin, was dendrimerized by two lysines at the C-terminal and was lipidated by n-butyric acid at the N-terminal, and thus exhibited the best antibacterial activity. However, the trimer had high hemolytic activity. Finally, A-C8, a simple structural lipopeptide, which is not a dendrimer, was obtained following the lipidation of anoplin using octanoic acid; it exhibited the highest therapeutic index, which makes it a probable antibiotic and thus was screened out.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
21
References
1
Citations
NaN
KQI