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Glycosyltransferase and its application to glycodiversification of natural products

机译:糖基转移酶及其在天然产物糖多样化中的应用

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摘要

Glycosyltransferase (GT) catalyzes the transfer of a sugar moiety to acceptor substrates such as secondary metabolites. The majority of GTs has two structural folds, GT-A and GT-B based on 3-D structural analysis. The limited structural fold diversity is compensated by a highly divergent acceptor binding domain for conferring sufficient substrate promiscuity. Various GTs have been engineered to further enhance the glucose transfer activity and expand substrate promiscuity by error-prone PCR and site-directed mutagenesis. Engineered GT-catalyzed glyeosylation will certainly play a key role in the generation of scaffold for new drug discovery and control of drug pharmacokinetics.
机译:糖基转移酶(GT)催化糖部分向受体底物(例如次级代谢产物)的转移。根据3-D结构分析,大多数GT具有两个结构折叠,即GT-A和GT-B。有限的结构折叠多样性被高度发散的受体结合域所补偿,以赋予足够的底物混杂性。通过易于出错的PCR和定点诱变,已设计了各种GT,以进一步增强葡萄糖转移活性并扩大底物混杂。工程的GT催化的糖基化肯定会在新药物发现和药物药代动力学控制的支架产生中发挥关键作用。

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