Bacterial 2-component signal transduction systems: A fluorescence polarization screen for response regulator-protein binding
Bacterial 2-component signal transduction systems: A fluorescence polarization screen for response regulator-protein binding
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DOI：
10.1177/1087057104273930
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发表时间：
2005-04-01
影响因子：
--
通讯作者：
Weisblum, B
中科院分区：
文献类型：
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作者：
Erickson, MG;Ulijasz, AT;Weisblum, B
双组分信号转导系统是细菌感知环境变化并整合适应性反应的主要手段。在病原菌中，双组分信号转导（TCST）激酶参与毒力和抗生素抗性的表达。这使得细菌TCST系统成为药物干预的有吸引力的靶标。本文描述了一种荧光偏振分析，定量细菌DNA启动子片段和它们的同源反应调节蛋白之间的结合。使用来自屎肠球菌的VanRSTCST系统（其编码万古霉素抗性），作者证明了反应调节蛋白/启动子片段与已知抑制剂结合的抑制。所观察到的结合常数与表面等离子体共振测量中报道的结合常数相当，并得到位移测量。（Journal of Biomolecular Screening 2005：270-274）。
Two-component signal transduction systems are the primary means by which bacteria sense environmental change and integrate an adaptive response. In pathogenic bacteria, 2-component signal transduction (TCST) kinases are involved in the expression of virulence and antibiotic resistance. This makes bacterial TCST systems attractive targets for pharmacologic intervention. This paper describes a fluorescence polarization assay that quantifies the binding between bacterial DNA promoter segments and their cognate response regulator proteins. Using the VanRSTCST system from Enterococcus faecium, which encodes vancomycin resistance, the authors demonstrate inhibition of response regulator protein/promoter segment binding with a known inhibitor. Observed binding constants were comparable to those reported in surface plasmon resonance measurements and get shift measurements. (Journal of Biomolecular Screening 2005:270-274).