天然产物的糖基化及糖基侧链改造

抗生素和抗癌药物等多种天然产物的活性都依赖于其糖基侧链,糖基侧链结构的变化对母体化合物的生物活性、底物适应性及药理学性质具有重要影响。糖基侧链结构变化多端,修饰、改变天然产物的糖基侧链已成为获得临床候选药物的重要方法。利用化学法和酶法,研究者创造了多种改造天然产物糖基化的方法。详细介绍了天然产物的糖基化过程,并从组合生物学、糖基转移酶改造、糖类随机化及新型糖类随机化和糖基转移酶可逆性四方面阐述了糖基侧链的改造方法。

Natural Product Glycosylation and Aglycone Diversifcation

The bioactivity of many natural products including antibiotics and anticancer therapeutics depends on their sugar moieties.Changes in the structures of these sugars can deeply influence the biological activity,specificity and pharmacological properties of the parent compounds.A unique characteristic of sugar moieties is their structural diversity which is greater than that of many other biological compounds.Modification of these parts has become an important strategy to achieve many clinical drug candidates.Research groups have focused upon the development of chemical and enzymatic tools to diversity natural product glycosylation.The glycosylation process of natural products and four strategy to diversity glycosylation were discussed in detail.