Department of Chemistry, Biochemistry, and Pharmaceutical Sciences, University of Bern, Freiestrasse 3, CH-3012 Bern, Switzerland.
School of Chemistry, University of Nottingham, University Park, NG7 2RD, Nottingham, UK.
Chem Commun (Camb). 2022 Oct 27;58(86):12118-12121. doi: 10.1039/d2cc04660a.
In order to expand the toolbox of enzymes available for thioglycoside synthesis, we describe here the first example of an extremophilic glycosyl hydrolase from (GH1) engineered towards thioglycosynthase activity with a novel combination of mutations. Using the triple mutant, GH1 M299R/E166A/E354G, a range of thioglycosides from glycosyl fluoride donors and aromatic thiols could be synthesised with exquisite stereoselectivity and good to excellent conversions (61-93%).
为了拓展可用于硫代糖合成的酶工具，我们在此描述了首例经新型突变组合工程化的嗜极糖苷水解酶（GH1），使其向硫代糖合成酶活性转变。利用三重突变体 GH1 M299R/E166A/E354G，可从糖基氟供体和芳香硫醇合成一系列硫代糖苷，具有极好的立体选择性和良好到优秀的转化率（61-93%）。
