| 结核分枝杆菌泛酸合成酶抑制剂的实验研究 |
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| 引用本文： | 杨延辉,刘忆霜,关艳,郝雪秦,龚立康,肖春玲. 结核分枝杆菌泛酸合成酶抑制剂的实验研究[J]. 中国新药杂志, 2011, 0(12) |
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| 作者姓名： | 杨延辉 刘忆霜 关艳 郝雪秦 龚立康 肖春玲 |
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| 作者单位： | 北京协和医学院中国医学科学院医药生物技术研究所; |
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| 基金项目： | 国家“重大传染病防治”科技重大专项(2008ZX10003-006) |
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| 摘 要： | 目的:获得特异性靶向结核分枝杆菌泛酸合成酶的抑制剂,为开发针对该靶点的新型抗结核药物奠定基础。方法:重组表达结核分支杆菌H37Rv的泛酸合成酶,以酶活测定体系为基础构建高通量筛选模型,对筛选到的酶抑制剂进行酶促动力学研究,并运用分枝杆菌微量直观快速药敏试验法测定其体外抗结核活性。结果:得到了具有天然活性的泛酸合成酶,建立并优化了酶活测定体系及筛选模型,应用模型筛选得到了具有新结构的抑制剂。评价结果显示,该抑制剂具有显著的体外抗结核活性。结论:获得了具有显著体外抗结核活性的新型泛酸合成酶抑制剂。
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| 关 键 词： | 结核分枝杆菌 泛酸合成酶 抑制剂 高通量筛选 |
A study on novel inhibitors of mycobacteria tuberculosis pantothenate synthetase |
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| YANG Yan-hui,LIU Yi-shuang,GUAN Yan,HAO Xue-qin,GONG Li-kang,XIAO Chun-ling. A study on novel inhibitors of mycobacteria tuberculosis pantothenate synthetase[J]. Chinese Journal of New Drugs, 2011, 0(12) |
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| Authors: | YANG Yan-hui LIU Yi-shuang GUAN Yan HAO Xue-qin GONG Li-kang XIAO Chun-ling |
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| Affiliation: | YANG Yan-hui,LIU Yi-shuang,GUAN Yan,HAO Xue-qin,GONG Li-kang,XIAO Chun-ling(Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China) |
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| Abstract: | Objective: To discover novel inhibitors specially targeting Mycobacteria tuberculosis(MTB) pantothenate synthetase(PS),and provide a foundation for the development of novel antitubercular drugs.Methods: The PS of MTB H37Rv was cloned,expressed,and purified.The screening system was build based on the assay of enzyme activity.The potential inhibitors were screened.The enzyme kinetics of lead hit was studied.The antitubercular activity was evaluated by the micro-assay of MTB with celerity and sensitivity.Resul... |
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| Keywords: | Mycobacterium tuberculosis pantothenate synthetase inhibitor high-throughput screening |
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