放线菌天然产物糖基化改造研究进展

Engineering the glycosylation pattern of natural products in actinobacteria

摘要:

放线菌可以产生结构多样的天然产物, 其中包括很多重要的抗菌和抗肿瘤药物。糖基化修饰在天然产物中广泛存在, 糖基侧链的变化往往会影响天然产物的生物活性。本文综述了放线菌来源天然产物糖基化改造的研究进展。糖基侧链改造的方法主要分为体内基因工程和体外酶学法。运用这两种方法已经成功对多种天然产物进行了糖基侧链改造, 获得了大量带有新糖基修饰的天然产物, 其中有些生物活性得以提高。天然产物糖基侧链改造为新药开发提供了一个重要的途径。

Abstract:

Actinobacteria are known to produce various natural products, including many important antibacterial and antitumor antibiotics. Glycosylation is a common tailoring reaction in natural product biosynthesis. In most cases, glycosylation significantly affects the bioactivity of natural products. The glycosylation of natural products could be manipulated by in vivo genetic engineering or by in vitro enzymatic glycodiversification approaches. A large number of new glycosylated products were generated using these two approaches, and some of them showed enhanced bioactivity. These new glycosyl-diversified products offer new opportunities for drug development.