State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences , Peking University , 38 Xueyuan Road , Beijing 100191 , China.
Hefei National Laboratory for Physical Science at Microscale and School of Life Sciences , University of Science and Technology of China , Hefei 230026 , China.
Org Lett. 2019 Apr 5;21(7):2241-2245. doi: 10.1021/acs.orglett.9b00524. Epub 2019 Mar 8.
A highly regio-specific and donor-promiscuous 3- O-glycosyltransferase, Sb3GT1 (UGT78B4), was discovered from Scutellaria baicalensis. Sb3GT1 could accept five sugar donors (UDP-Glc/-Gal/-GlcNAc/-Xyl/-Ara) to catalyze 3- O-glycosylation of 17 flavonols, and the conversion rates could be >98%. Five new glycosides were obtained by scaled-up enzymatic catalysis. Molecular modeling and site-directed mutagenesis revealed that G15 and P187 were critical catalytic residues for the donor promiscuity. Sb3GT1 could be a promising catalyst to increase structural diversity of flavonoid 3- O-glycosides.
从黄芩中发现了一个高度区域特异性和供体混杂的 3-O-糖基转移酶 Sb3GT1（UGT78B4）。Sb3GT1 可以接受五种糖供体（UDP-Glc/-Gal/-GlcNAc/-Xyl/-Ara），催化 17 种黄酮醇的 3-O-糖基化反应，转化率可>98%。通过扩大酶催化获得了五个新的糖苷。分子建模和定点突变揭示 G15 和 P187 是供体混杂的关键催化残基。Sb3GT1 可能是增加黄酮 3-O-糖苷结构多样性的有前途的催化剂。
