Effect of Modification Strategies on the Biological Activity of Peptides/Proteins

Covalent attachment of biologically active peptides/proteins with functional moieties is an effective strategy to control their biodistribution, pharmacokinetics, enzymatic digestion, and toxicity. This review focuses on the characteristics of different modification strategies and their effects on the biological activity of peptides/proteins and illustrates their relevant applications and potential. This review focuses on PEGylation, N-terminal acetylation, glycosylation, and some other modifications of peptide/proteins. Characteristics of structures for modifying groups and improvement of the peptide/proteins' properties including their biodistribution, pharmacokinetics, enzymatic digestion, and toxicity were discussed. Some typical examples relating to regulating biological activities or critical physiological processes were illustrated for different peptide/proteins' modifications.image