The pegylated proteins and peptides have found promising applications in biotechnological and biomedical fields due to the improved solubility, thermal and mechanical stability, reduced antigenicity and immunogenicity, enhanced circulating half-lives, optimized pharmacokinetic and pharmacodynamic properties. Consequently, pegylation gradually becomes a platform technology. The importance of chemistry of protein and peptide pegylation has attracted more and more attentions as more PEG-conjugates have reached late phase clinical trials. In this paper, the first-generation and second- generation pegylation chemistry is briefly reviewed, mainly including the different types of PEG chemical modifiers and their performance comparison.

Key words: PROTEIN, PEPTIDE, POLYGLYCOL, CHEMICLAL MODIFICATION