Novel DNA Topoisomerase IIα Inhibitors from Combined Ligand- and Structure-Based Virtual Screening

@inproceedings{Drwal2014NovelDT,
  title={Novel DNA Topoisomerase IIα Inhibitors from Combined Ligand- and Structure-Based Virtual Screening},
  author={Malgorzata N. Drwal and Jessica Marinello and Stefano Giustino Manzo and Laurence P. G. Wakelin and Giovanni Capranico and Renate Griffith},
  booktitle={PloS one},
  year={2014}
}
DNA topoisomerases are enzymes responsible for the relaxation of DNA torsional strain, as well as for the untangling of DNA duplexes after replication, and are important cancer drug targets. One class of topoisomerase inhibitors, "poisons", binds to the transient enzyme-DNA complex which occurs during the mechanism of action, and inhibits the religation of DNA. This ultimately leads to the accumulation of DNA double strand breaks and cell death. Different types of topoisomerases occur in human… CONTINUE READING
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