Thiabendazole inhibits ubiquinone reduction activity of mitochondrial respiratory complex Ⅱ via a water molecule mediated binding feature  

作　　者：Qiangjun Zhou Yujia Zhai Jizhong Lou Man Liu Xiaoyun Pang Fei Sun 

机构地区：[1]National Laboratory of Biomacromolecules,Institute of Biophysics,Chinese Academy of Sciences,Beijing 100101,China [2]Graduate School of the Chinese Academy of Sciences,Beijing 100080,China

出　　处：《Protein & Cell》2011年第7期531-542,共12页蛋白质与细胞（英文版）

基　　金：supported by grants from the National Basic Research Program(973 Program)(Nos.2011CB910301,2011CB910900,and 2006CB806506);the National Natural Science Foundation of China(Grant No.31021062).

摘　　要：The mitochondrial respiratory complex Ⅱ or succinate:ubiquinone oxidoreductase(SQR)is a key membrane complex in both the tricarboxylic acid cycle and aerobic respiration.Five disinfectant compounds were investigated with their potent inhibition effects on the ubiquinone reduction activity of the porcine mitochondrial SQR by enzymatic assay and crystallography.Crystal structure of the SQR bound with thiabendazole(TBZ)reveals a different inhibitor-binding feature at the ubiquinone binding site where a water molecule plays an important role.The obvious inhibitory effect of TBZ based on the biochemical data(IC50~100μmol/L)and the significant structure-based binding affinity calculation(~94μmol/L)draw the suspicion of using TBZ as a good disinfectant compound for nematode infections treatment and fruit storage.

关 键 词：mitochondrial respiratory complexⅡ THIABENDAZOLE PENTACHLOROPHENOL inhibition CRYSTALLOGRAPHY 

分 类 号：O62[理学—有机化学]