abstract |
The present invention provides a modification method and application of a polypeptide. The method includes the following steps: (1) introducing X into the N-terminal of the polypeptide to obtain an X-polypeptide; (2) oxidizing the X to an aldehyde group; (3) ) adding a reducing agent, and covalently coupling the oxidized product obtained in step (2) with PEG to obtain a PEG-modified polypeptide; wherein, the X is threonine or serine. In the present invention, a threonine or a serine is introduced into the N-terminus of the polypeptide, and a highly specific oxidation method is used to derivatize the adjacent aminoalcohol structure at the N-terminus of the polypeptide into an aldehyde group, and after covalent coupling with PEG, a single-component PEG is obtained. The modified polypeptide has strong versatility and wide application range, and the modified polypeptide has a simple and convenient separation method, which improves the stability and circulation half-life of the polypeptide. |