中文摘要：

在临床上得到广泛应用的大环内酯类抗生素的合成中，糖基化反应对其发挥生物功能十分重要，同时大环内酯糖基化也是一种微生物产生抗生素抗性的重要手段。这些糖基化反应是由一种被称为糖基转移酶（GTase）的蛋白催化完成的，对大环内酯GTase结构、功能和应用领域的研究将为组合生物学研究奠定坚实的基础。本文详细介绍了大环内酯糖基化的生物功能，并对大环内酯GTase的分类和发现情况作了深入讨论。随后回顾了大环内酯糖基化产生的抗性机制，并对相应的GTase MGT进行了细致的介绍。依据大环内酯GTase具有灵活底物特异性的特点，认真总结了其在组合生物学领域的应用情况。最后，作者根据本课题组的相关研究成果，对大环内酯GTase的应用前景进行了展望。

英文摘要：

Catalyzed by a family of enzymes called glycosyltransferases （GTases）, glycosylation reactions are essential for the bioactivities of macrolide antibiotics which have been widely applied. Additionally, glycosylation is also an important strategy of microbial to get macrolide antibiotic resistance. Studies on the structure, function and application areas of macrolide GTases will lay the stable groundwork for the combinatorial biology. This paper introduced in detail the biological functions of macrolide glycosylation, and then made an in-depth discussion on the families and discoveries of macrolide GTases. The resistance mechanism with macrolide glycosyhion and the correlative GTases MGT have been reviewed afterwards. According to the flexible substrate specificity of macrolide GTases, the combinatorial biological applications on them were also seriously summarized here. At the end, the authors made a developmental prospect of macrolide GTases based on the studies of the research group.