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The Effect of the Potential PhoQ Histidine Kinase Inhibitors on Shigella flexneri Virulence

文献类型：期刊论文

作者Cai, Xia2,3,4; Zhang, Jian5; Chen, Mingliang1; Wu, Yang2,3,4; Wang, Xueqing2,3,4; Chen, Jiayu2,3,4; Zhang, Junqin2,3,4; Shen, Xu5; Qu, Di2,3,4; Jiang, Hualiang5
刊名PLOS ONE
出版日期2011-08-10
卷号6期号:8
ISSN号1932-6203
DOI10.1371/journal.pone.0023100
文献子类Article
英文摘要PhoQ/PhoP is an important two-component system that regulates Shigella virulence. We explored whether the PhoQ/PhoP system is a promising target for new antibiotics against S. flexneri infection. By using a high-throughput screen and enzymatic activity coupled assay, four compounds were found as potential PhoQ inhibitors. These compounds not only inhibited the activity of SF-PhoQc autophosphorylation but also displayed high binding affinities to the SF-PhoQc protein in the Surface Plasmon Resonance response. A S. flexneri cell invasion assay showed that three of these potential PhoQ inhibitors inhibit the invasion of HeLa cells by S. flexneri 9380. In a Mouse Sereny test, mice inoculated with S. flexneri 9380 pre-treated with the potential PhoQ inhibitors 1, 2, 3 or 4 displayed no inflammation, whereas mice inoculated with S. flexneri 9380 alone displayed severe keratoconjunctival inflammation. All four potential PhoQ inhibitors showed no significant cytotoxicity or hemolytic activity. These data suggest that the four potential PhoQ inhibitors inhibited the virulence of S. flexneri and that PhoQ/PhoP is a promising target for the development of drugs against S. flexneri infection.
WOS关键词2-COMPONENT REGULATORY SYSTEM ; QUORUM-SENSING INHIBITORS ; BACTERIAL SENSOR KINASE ; ESCHERICHIA-COLI ; PSEUDOMONAS-AERUGINOSA ; SIGNAL-TRANSDUCTION ; ANTIMICROBIAL PEPTIDES ; SEROVAR TYPHIMURIUM ; ACETYL PHOSPHATE ; SMALL MOLECULES
资助项目Ministry of Science and Technology of China[2009ZX09303-005] ; Ministry of Science and Technology of China[2008ZX10003-016] ; Ministry of Science and Technology of China[2010DFA32100] ; National Natural Science Foundation of China[30800036] ; National Natural Science Foundation of China[J0730860] ; Scientific Technology Development Foundation of Shanghai[10410700600] ; Scientific Technology Development Foundation of Shanghai[09DZ1908602] ; Scientific Technology Development Foundation of Shanghai[08JC1401600] ; Fudan University[09FQ43]
WOS研究方向Science & Technology - Other Topics
语种英语
WOS记录号WOS:000295454200042
出版者PUBLIC LIBRARY SCIENCE
源URL[http://119.78.100.183/handle/2S10ELR8/278443]  
专题药物发现与设计中心
通讯作者Cai, Xia
作者单位1.Shanghai Municipal Ctr Dis Control & Prevent, Shanghai, Peoples R China
2.Fudan Univ, Inst Med Microbiol, Minist Hlth, Key Lab Med Mol Virol, Shanghai 200433, Peoples R China;
3.Fudan Univ, Inst Biomed Sci, Shanghai 200433, Peoples R China;
4.Fudan Univ, Inst Med Microbiol, Minist Educ, Key Lab Med Mol Virol, Shanghai 200433, Peoples R China;
5.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med,Grad Sch, Drug Discovery & Design Ctr,State Key Lab Drug Re, Shanghai, Peoples R China;
推荐引用方式
GB/T 7714		 Cai, Xia,Zhang, Jian,Chen, Mingliang,et al. The Effect of the Potential PhoQ Histidine Kinase Inhibitors on Shigella flexneri Virulence[J]. PLOS ONE,2011,6(8).
APA Cai, Xia.,Zhang, Jian.,Chen, Mingliang.,Wu, Yang.,Wang, Xueqing.,...&Jiang, Hualiang.(2011).The Effect of the Potential PhoQ Histidine Kinase Inhibitors on Shigella flexneri Virulence.PLOS ONE,6(8).
MLA Cai, Xia,et al."The Effect of the Potential PhoQ Histidine Kinase Inhibitors on Shigella flexneri Virulence".PLOS ONE 6.8(2011).

入库方式： OAI收割

来源：上海药物研究所

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