...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Bioorganic and Medicinal Chemistry >Disaccharide analogs as probes for glycosyltransferases in Mycobacterium tuberculosis
【24h】

Disaccharide analogs as probes for glycosyltransferases in Mycobacterium tuberculosis

机译：二糖类似物作为结核分枝杆菌糖基转移酶的探针

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Glycosyltransferases (GTs) play a crucial role in mycobacterial cell wall biosynthesis and are necessary for the survival of mycobacteria. Hence, these enzymes are potential new drug targets for the treatment of tuberculosis (TB), especially multiple drug-resistant TB (MDR-TB). Herein, we report the efficient syntheses of Araf(α 1 → 5)Araf, Galf(β 1 → 5)Galf, and Galf(β 1 → 6)Galf disaccharides possessing a 5-N,N-dimethylaminonaphthalene-1-sulfonamidoethyl (dansyl) unit that were prepared as fluorescent disaccharide acceptors for arabinosyl- and galactosyl-transferases, respectively. Such analogs may offer advantages relative to radiolabeled acceptors or donors for studying the enzymes and for assay development and compound screening. Additionally, analogs possessing a 5-azidonaphthalene-1-sulfonamidoethyl unit were prepared as photoaffmity probes for their potential utility in studying active site labeling of the GTs (arabinosyl and galactosyl) in Mycobacterium tuberculosis (MTB). Beyond their preparation, initial biological testing and kinetic analysis of these disaccharides as acceptors toward glycosyltransferases are also presented.
机译：糖基转移酶（GTs）在分枝杆菌细胞壁生物合成中起关键作用，对于分枝杆菌的生存是必需的。因此，这些酶是治疗结核病（TB），尤其是多重耐药结核病（MDR-TB）的潜在新药靶标。在本文中，我们报告了具有5-N，N-二甲基氨基萘-1-磺酰胺基乙基（5-N，N-二甲基氨基萘-1-磺酰胺基）的Araf（α1→5）Araf，Galf（β1→5）Galf和Galf（β1→6）Galf二糖的有效合成方法。 dansyl）单元，分别用作阿拉伯糖基和半乳糖基转移酶的荧光二糖受体。相对于放射性标记的受体或供体，此类类似物可提供用于研究酶以及用于分析开发和化合物筛选的优势。另外，制备具有5-叠氮基萘-1-磺酰胺基乙基单元的类似物作为光亲和性探针，因为它们在研究结核分枝杆菌（MTB）中的GT（阿拉伯糖基和半乳糖基）的活性位点标记中具有潜在的实用性。除了它们的制备以外，还介绍了这些二糖作为糖基转移酶受体的初步生物学测试和动力学分析。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号