改造糖基侧链合成新型抗生素的研究进展

Advances in synthesis of new antibiotics by modifying glycosyl chains

放线菌抗生素核心结构普遍存在糖基化,糖基在抗生素药理作用的发挥中起到了非常重要的作用。随着抗生素糖基合成基因簇研究的深入,运用现代基因工程技术,借助糖基转移酶的底物灵活性,已实现了多种抗生素糖基侧链的改造,进而合成新结构的抗生素。文中详细介绍了目前抗生素糖基侧链改造的主要方法,以及运用基因工程技术对糖类合成途径进行调控以产生新型糖基化衍生物的研究进展。

Antibiotics produced by actinomycetes are frequently glycosylated with saccharide chains, in which the sugars contribute to specific pharmacological actions of the antibiotics. With the further understanding of sugar biosynthesis pathways, many new antibiotics have been produced by means of genetic engineering approaches in antibiotic-producing actinomycetes via generating derivatives with novel sugars in their architecture. In this review, we introduced in detail the means of saccharide chains＇reconstruction, and discussed the recent progress in the novel glycosylated derivatives generated from natural products by genetic engineering through the sugar biosynthesis pathways.