蛋白质多肽药物聚乙二醇定点修饰的研究进展

The research progress of protein and peptide site-PEGylation

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。

PEGylation of proteins and peptides could resolve many problems such as increasing solubility, enhancing stability, prolonging half-lives, reducing toxicity and shielding immunogenic epitopes. The progress of site-PEGylation for amino, thiol, carboxyl and oxidized aldehyde groups are reviewed.