Intramolecular cyclization of the antimicrobial peptide Polybia ‐MPI with triazole stapling: influence on stability and bioactivity

In conclusion, the design and synthesis of cyclic analogs via click chemistry offer a new strategy for the development of stable antimicrobial agents. Copyright © 2017 European Peptide Society and John Wiley & Sons, Ltd. The MPI cyclic analogs C‐MPI‐1 (i‐ to ‐i+4) and C‐MPI‐2 (i‐ to ‐i+6) were synthesized by copper(I)‐catalyzed azide‐alkyne cycloaddition. Cyclic analogs have different bioactivity, and especially, C‐MPI‐1 has enhanced anti‐trypsin resistance compared with the parent peptide MPI. The mechanism of action and the secondary structure of all peptides were further investigated.
Source: Journal of Peptide Science - Category: Biochemistry Authors: Tags: Research Article Source Type: research