聚乙二醇（PEG）修飾是解決蛋白質(zhì)藥物溶解度低、穩(wěn)定性差、半衰期短、具有免疫原性等問(wèn)題的有效方法，通常在氨基上進(jìn)行修飾，但在巰基上進(jìn)行定點(diǎn)修飾更有利于獲得結(jié)構(gòu)明確、組成穩(wěn)定的修飾產(chǎn)物。綜述了聚乙二醇定點(diǎn)修飾蛋白質(zhì)藥物中巰基，包括在游離巰基、二硫鍵和引入的巰基上進(jìn)行修飾的研究進(jìn)展。

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.

天津市科技計(jì)劃項(xiàng)目（15PTSYJC00220）