Document Detail

Potent in vitro Interference of Fleroxacin in DNA-binding, Unwinding and ATPase Activities of Bloom Helicase.
MedLine Citation:
PMID:  23534463     Owner:  NLM     Status:  In-Data-Review    
OBJECTIVE: To study the effect of fleroxacin (FLRX) on biological properties of Bloom (BLM) helicase catalytic core (BLM642-1290 helicase) in vitro and the molecular mechanism of interaction between the two molecules.
METHODS: DNA-binding and unwinding activities of BLM642-1290 helicase were assayed by fluorescence polarization and gel retardation assay under conditions that the helicase was subjected to different concentrations of FLRX. Effect of FLRX on helicase ATPase activity was analyzed by phosphorus-free assay based on a colorimetric estimation of ATP hydrolysis-produced inorganic phosphate. Molecular mechanism of interaction between the two molecules was assayed by ultraviolet and fluorescence spectra.
RESULTS: The DNA unwinding and ATPase activities of BLM642-1290 helicase were inhibited whereas the DNA-binding activity was promoted in vitro. A BLM-FLRX complex was formed through one binding site, electrostatic and hydrophobic interaction force. Moreover, the intrinsic fluorescence of the helicase was quenched by FLRX as a result of non-radioactive energy transfer. The biological activity of helicase was affected by FLRX, which may be through an allosteric mechanism and stabilization of enzyme conformation in low helicase activity state, disruption of the coupling of ATP hydrolysis to unwinding, and blocking helicase translocation on DNA strands.
CONCLUSION: FLRX may affect the biological activities and conformation of BLM642-1290 helicase, and DNA helicase may be used as a promising drug target for some diseases.
Heng Luo; Hou Qiang Xu; Xiang Chen; Mei Ding; Qi Xin Yang; Kun Li
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Biomedical and environmental sciences : BES     Volume:  26     ISSN:  0895-3988     ISO Abbreviation:  Biomed. Environ. Sci.     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-03-28     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8909524     Medline TA:  Biomed Environ Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  231-42     Citation Subset:  IM    
Copyright Information:
Copyright © 2013 The Editorial Board of Biomedical and Environmental Sciences. Published by China CDC. All rights reserved.
Key Laboratory of Animal Genetics, Breeding and Reproduction in Plateau Mountainous Region, Ministry of Education, College of Animal Science, Guizhou University, Guiyang 550025, Guizhou, China; Guizhou Key Laboratory of Animal Genetics, Breeding and Reproduction, College of Animal Science, Guizhou University, Guiyang 550025, Guizhou, China; Provincial Key Laboratory for Agricultural Pest Management of Mountainous Region, Guizhou University, Guiyang 550025, Guizhou, China.
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