Site-selective editing of peptides via backbone modification

The site-selective editing of peptides and proteins through backbone modification holds significant promise in the realms of therapeutic and diagnostic agents, drug development, and biological tool compounds. Even subtle alterations within the peptide skeleton can profoundly influence the overall properties of the peptide. This comprehensive review delves into various modification protocols applied to peptides and proteins, encompassing direct N-functionalization of peptide bonds, selective formation of heterocyclic units in the backbone, N-terminal modification of peptide skeletons, and cleavage of peptide skeletons. While reports on selective peptide skeleton modification remain limited, the field is poised for significant growth and development in the coming years.