Structural insight into the oxidation-sensing mechanism of the antibiotic resistance of regulator MexR
Structural insight into the oxidation-sensing mechanism of the antibiotic resistance of regulator MexR
复制标题
调节剂 MexR 抗生素耐药性氧化传感机制的结构洞察
DOI：
10.1038/embor.2010.96
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发表时间：
2010-09-01
期刊：
影响因子：
7.7
通讯作者：
He, Chuan
中科院分区：
文献类型：
--
作者：
Chen, Hao;Yi, Chengqi;He, Chuan
MexR作为铜绿假单胞菌中mexAB-oprM多药外排表达的主要调节因子发挥作用。已经表明，MexR通过在氧化还原活性半胱氨酸之间形成蛋白质间二硫键来感测氧化应激。这种氧化诱导MexR从启动子DNA解离，从而激活外排泵基因的转录表达。在这项研究中，我们提出了MexR在其氧化形式的晶体结构在2.1埃的分辨率。这种晶体结构揭示了氧化信号变构去抑制MexR控制的转录激活的机制。
MexR functions as the primary regulator of the mexAB-oprM multidrug efflux expression in Pseudomonas aeruginosa. It has been shown that MexR senses oxidative stress by interprotomer disulphide bond formation between redox-active cysteines. This oxidation induces MexR to dissociate from the promoter DNA, thus activating the transcriptional expression of efflux pump genes. In this study, we present the crystal structure of MexR in its oxidized form at a resolution of 2.1 angstrom. This crystal structure reveals the mechanism by which oxidative signal allosterically derepresses the MexR-controlled transcription activation.