Regioselective C-H hydroxylation of omeprazole sulfide by Bacillus megaterium CYP102A1 to produce a human metabolite
Regioselective C-H hydroxylation of omeprazole sulfide by Bacillus megaterium CYP102A1 to produce a human metabolite
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DOI：
10.1007/s10529-016-2211-3
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发表时间：
2017-01-01
影响因子：
2.7
通讯作者：
Yun, Chul-Ho
中科院分区：
文献类型：
--
作者：
Jang, Hyun-Hee;Ryu, Sang-Hoon;Yun, Chul-Ho
以廉价的底物奥美拉唑硫化物为原料，寻找一种简单的酶促合成5‘-羟基奥美拉唑硫化物的方法，通过从高转化率的CYP102A1文库中蓝菌落筛选获得一组高活性的CYP102A1突变体，实现了5’-羟基奥美拉唑硫化物的合成。该突变酶甚至野生型酶催化奥美拉唑硫化物高区域选择性(98%)C-H羟基化合成5‘-羟基奥美拉唑硫化物，转化率高(85-90%)。
To find a simple enzymatic strategy for the efficient synthesis of the expensive 5'-hydroxyomeprazole sulfide, a recently identified minor human metabolite, from omeprazole sulfide, which is an inexpensive substrate.The practical synthetic strategy for the 5'-OH omeprazole sulfide was accomplished with a set of highly active CYP102A1 mutants, which were obtained by blue colony screening from CYP102A1 libraries with a high conversion yield. The mutant and even the wild-type enzyme of CYP102A1 catalyzed the high regioselective (98 %) C-H hydroxylation of omeprazole sulfide to 5'-OH omeprazole sulfide with a high conversion yield (85-90 %).A highly efficient synthesis of 5'-OH omeprazole sulfide was developed using CYP102A1 from Bacillus megaterium as a biocatalyst.