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微生物及其酶催化的天然产物糖基化反应
引用本文:刘爽, 李凯, 王双, 乔雪, 叶敏. 微生物及其酶催化的天然产物糖基化反应[J]. 药学进展, 2018, 42(1): 14-20.
作者姓名:刘爽  李凯  王双  乔雪  叶敏
作者单位:1.北京大学药学院天然药物及仿生药物国家重点实验室,北京 100191
摘    要:

天然产物具有广泛的生物活性,是新药发现的重要来源。然而很多天然产物活性不够强、溶解性差、生物利用度低,需要通过结构修饰提高成药性。糖基化是一种重要的结构修饰反应。微生物催化具有选择性强、反应条件温和、环境友好等特点。对微生物全细胞及重组表达酶催化的天然产物糖基化反应的最新进展进行综述。



关 键 词:天然产物  微生物  糖基转移酶  糖苷酶  糖基化

Natural products as sources of new drugs from 1981 to 2014
LIU Shuang, LI Kai, WANG Shuang, QIAO Xue, YE Min. Glycosylation of Natural Products Catalyzed by Microorganisms and Their Enzymes[J]. Progress in Pharmaceutical Sciences, 2018, 42(1): 14-20.
Authors:LIU Shuang  LI Kai  WANG Shuang  QIAO Xue  YE Min
Affiliation:1.State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Abstract:As an important source of new drugs, natural products exhibit extensive biological activities. However, most of them suffer from less potent activity, poor water solubility, and low bioavailability. Consequently, structural modification is needed to improve their druggability. Glycosylation is an important reaction for structural modification. Microbial transformation has the advantages of high selectivity, mild reaction conditions, and environmental friendliness. The recent progress in the field of glycosylation of natural products catalyzed by both whole cells and recombinant enzymes of microorganisms were reviewed.
Keywords:natural product  microorganism  glycosyltransferase  glycosidase  glycosylation
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