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Potent interference of DNA unwinding, ATPase and DNA-binding activities of Bloom helicase by Fleroxacin
LUO Heng 1,XU Houqiang 2 *,CHEN Xiang 3,DING Mei 4,YANG Qixin 5,XU Qinghe 4,LIU Jinhe 2
1.Key Laboratory of Animal Genetics,Breeding and Reproduction in the Plateau Mountainous Region,Ministry of Education,College of animal science,Guizhou University, GuiYang 550025
2. Guizhou Key Laboratory of Animal Genetics, Breeding and Reproduction, College of animal science, Guizhou University, Guiyang 550025, China
3. The Provincial Key Laboratory for Agricultural Pest Management of Mountainous Region, Guizhou University, Huaxi, Guiyang, 550025, China
4.Key Laboratory of Animal Genetics,Breeding and Reproduction in the Plateau Mountainous Region,Ministry of Education,College of animal science,Guizhou University,Guiyang,550025,China
5.Guizhou Key Laboratory of Animal Genetics, Breeding and Reproduction, College of animal science, Guizhou University, Guiyang 550025, China
*Correspondence author
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Funding: The authors are grateful for financial support from National Basic Research Program of China (No.No.2010CB534912), the Doctoral Program of the Ministry of Education(No.No.200806570003), Guizhou University innovation funds of graduate student (No.No.SYN 2009005), the Governor of Guizhou Province Talents Fund(No.No.200822)
Opened online:20 March 2012
Accepted by: none
Citation: LUO Heng,XU Houqiang,CHEN Xiang.Potent interference of DNA unwinding, ATPase and DNA-binding activities of Bloom helicase by Fleroxacin[OL]. [20 March 2012] http://en.paper.edu.cn/en_releasepaper/content/4471140
 
 
Bloom (BLM) helicase plays an important role in the processes of DNA metabolism including DNA replication, repair, transcription, and recombination. Fleroxacin (FLRX), an important antibiotic applied in the empirical treatment of a variety of infections, has currently been used as the effective drugs for anti-cancer therapy. This study was conducted to determine the effects of FLRX on the biological properties of BLM helicase catalytic core by fluorescence polarization, spectroscopy, free-phosphorus assay, and gel retardation assay. Results indicated that the DNA unwinding and ATPase activities were inhibited by FLRX treatment. However, the DNA-binding activity was promoted. BLM-FLRX complex was form through one binding site, electrostatic force, and hydrophobic interaction force. Moreover, the intrinsic fluorescence of the helicase was statically quenched by FLRX as a result of non-radioactive energy transfer. The results suggested that FLRX may affect the biological activities and conformation of the BLM helicase, which were beneficial to study the efficacy of DNA helicase as the target of drugs.
Keywords:BLM helicase; fleroxacin; biological activity
 
 
 

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