[关键词]
[摘要]
聚乙二醇(PEG)修饰是解决蛋白质药物溶解度低、稳定性差、半衰期短、具有免疫原性等问题的有效方法,通常在氨基上进行修饰,但在巯基上进行定点修饰更有利于获得结构明确、组成稳定的修饰产物。综述了聚乙二醇定点修饰蛋白质药物中巯基,包括在游离巯基、二硫键和引入的巯基上进行修饰的研究进展。
[Key word]
[Abstract]
Pegylation (PEG) is an effective way to overcome problems of protein drugs, such as low solubility, bad stability, short half-life, and having immunogenicity. Usually the modification is executed on amino, while the reaction based on thiol is more likely to obtain a product with clear structure and stable composition. Research progress on site-specific PEGylation on thiol in protein drugs, which included modifications on free thiol, double-sulfide bond, and imported thiol are reviewed in this paper.
[中图分类号]
[基金项目]
天津市科技计划项目(15PTSYJC00220)