A protein engineering strategy based on Focused Rational Iterative Site-specifi c Mutagenesis (FRISM) was developed in order to evolve mutants that allow for the fi rst time the glucosylation of polyhydroxy substrates such as silybin ( 1 ) with essentially complete regioselectivity, leading to the synthesis of pharmaceutically interesting products 2 , 3 and 4 , respectively. This approach also enables unusual N - and S -glucosylation.

中文翻译：

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糖基转移酶蛋白质工程的突破

为了发展突变体，该蛋白工程学策略是基于聚焦理性迭代特定位点诱变（FRISM）进行开发的，该突变体首次允许多羟基底物如水飞蓟宾（1）的糖基化具有基本完全的区域选择性，从而导致分别合成药学上感兴趣的产物2、3和4。这种方法还可以实现异常的N-和S-葡萄糖基化。