聚乙二醇修饰可以很好地解决蛋白多肽药物难溶性、稳定性差、半衰期短、毒性大、免疫原性等问题,其中的聚乙二醇定点修饰方式更具优势。本文着重介绍聚乙二醇在蛋白多肽药物中的N端氨基、巯基、羧基和糖类残基及N端氧化后的定点修饰方式的研究进展。 Polyethylene glycol modification can be a good solution to the poor solubility of protein peptide drugs, poor stability, short half-life, toxicity, immunogenicity and other issues, including polyethylene glycol fixed-point modification is more advantageous. This review focuses on the research progress of polyethylene glycol (PEG) in the site-directed modification of N-terminal amino, sulfhydryl, carboxyl and carbohydrate residues and N-terminal oxidation in protein peptide drugs.