Novel Protein PEGylation Chemistry via Glutalaldehyde-Functionalized PEG

Several PEGylated proteins have been approved as therapeutic drugs. In many cases, PEGylated protein has been synthesized by the conjugation reaction between PEG possessing activated ester and amine(s) in the protein. This reaction, however, often causes inactivation of PEGylated proteins. In this report, we present a novel chemistry which enables the PEGylation of proteins under the mild reaction condition. PEGylated lysozyme prepared by the method developed increased the biological activity of the PEGylated lysozyme more than 20 times compared with the PEGylated lysozyme prepared by the conventional method.