中文摘要：

糖基在微生物天然糖苷类抗生素的生物活性中扮演着重要角色，增减或者改变化合物的糖基构成往往会对化合物的生理活性产生决定性的影响。糖基的添加通常由糖基转移酶催化完成。本文综述了目前微生物天然糖苷类抗生素糖基转移酶的体外活性研究进展，阐述了糖基转移酶反应可逆性的发现，糖基转移酶辅助蛋白的重要性，以及糖基转移酶的体外糖基底物特异性的研究情况，并对将糖基转移酶应用于体外糖基多样化进行了展望。

英文摘要：

Sugar moieties play important roles in dictating the biological activities of microbial glycosidic antibiotics, which are largely affected by removing, adding or changing their sugar moieties. The attachment of sugar moieties are usually catalyzed by glycosyltransferases. This review provides an overview of recent progresses on the in vitro studies of glycosyltransferases from microbial glycosidic antibiotics, including their reverse catalysis, the requirement for an accessory protein, and their donor substrate flexibility. The perspective of glycosyltransferase for in vitro glycodiversification is discussed.