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Catalytic inhibition of topoisomerase II by a novel rationally designed ATP-competitive purine analogue

Patrick Chène1, Joëlle Rudloff1, Joseph Schoepfer2, Pascal Furet2, Peter Meier2, Zhiyan Qian1, Jean-Marc Schlaeppi3, Rita Schmitz3 and Thomas Radimerski1*

Author Affiliations

1 Department of Oncology, Novartis Institutes for BioMedical Research, Basel, Switzerland

2 Global Discovery Chemistry, Novartis Institutes for BioMedical Research, Basel, Switzerland

3 Biologics Center, Novartis Institutes for BioMedical Research, Basel, Switzerland

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BMC Chemical Biology 2009, 9:1  doi:10.1186/1472-6769-9-1

Published: 7 January 2009

Additional files

Additional File 1:

QAP 1 inhibits DNA decatenation mediated by purified human topoisomerase II alpha. Inhibition of purified human topoisomerase II alpha protein-mediated DNA decatenation in vitro by QAP 1. Lanes 1 and 10 (-Topo IIα): Samples in which the enzyme was omitted in the reaction. Lane 2 (+Topo IIα): DNA decatenation by purified enzyme and dose-dependent inhibition of the reaction by increasing concentrations of QAP 1 (lanes 3 – 9). Lane 11: DNA decatenation by purified topoisomerase II alpha enzyme is strictly dependent on the presence of ATP in the assay. The arrow marks the position of catenated kDNA substrate and the arrowheads designate the positions of decatenated kDNA topoisomerase II products, nicked circular and closed circular minicircles, respectively.

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