Engineering an Affinity-Enhanced Peptide through Optimization of Cyclization Chemistry.

ABSTRACT: Peptide cyclization is a strategy used to improve stability and activity of peptides. The most commonly used cyclization method is disulfide bridge formation of cysteine-containing peptides, as is typically found in nature. Over the years, an increasing number of alternative chemistries for peptide cyclization with improved efficiency, kinetics, orthogonality, and stability have been reported. However, there has been less appreciation for the opportunity to fine-tune peptide activity via the diverse chemical entities introduced at the site of linkage by different cyclization strategies. Here, we demonstrate how cyclization optimization of an M2 "anti-inflammatory" macrophage-binding peptide (M2pep) resulted in a significant increase in binding affinity of the optimized analog to M2 macroph

SUBMITTER: Ngambenjawong C 

PROVIDER: S-EPMC5678939 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature