蛋白质药物糖基化工程化改造研究进展

多种哺乳和非哺乳动物的蛋白质表达系统已成功用于重组糖蛋白药物的生产。糖基化对于生物药品的研究开发至关重要，对生物药品的药效、半衰期及抗原性等产生重要影响。糖基化工程的目的是生产组分明晰、结构均一的N-和O-连接的糖基化蛋白药物。N-糖基化改造的相关研究显示，利用哺乳动物和非哺乳动物表达系统可以表达均匀的N-聚糖重组糖蛋白。与N-糖基化改造相比， O-糖基化的改造研究尚处于起步阶段。首个糖基化工程单克隆抗体已在美国和日本获得上市批准。综述了重组蛋白表达系统的糖基化工程化改造的研究进展，包括蛋白质药物的 N-糖基化改造和O-糖基化改造的最新进展，以期为蛋白质药物的糖基化工程改造研究提供参考。

Research Progress of Glycosylation Engineering of Protein Drug

Mammalian and non-mammalian protein expression systems have been used in the production of recombinant glycoprotein drugs. Glycosylation is very important for the research and development of biopharmaceuticals, which has an important impact on its efficacy, half-life and antigenicity. The aim of glycosylation engineering is to produce N- and O-linked glycosylated protein drugs with clear components and uniform structure. Recent studies on N-glycosylation have shown that homogeneous recombinant N-glycans can be expressed in mammalian and non-mammalian expression systems. Compared with N-glycosylation, O-glycosylation is still in its infancy. The first glycosylation engineering monoclonal antibody has been approved for marketing in the United States and Japan. This paper reviewed the research progress of glycosylation engineering of recombinant protein expression system, including the progress on N-glycosylation and O-glycosylation, which was expected to provide reference for glycosylation engineering of protein drug research.