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The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs

AuthorsCanals, Albert ; Purciolas, Mònica; Aymamí, Joan; Coll, Miquel
Keywordsanticancer drugs
intercalating agent
ellipticine derivative
antineoplastic agent
DNA binding
drug design
Issue Date4-Jul-2005
PublisherBlackwell Publishing
CitationActa Crystallographica Section D: Biological Crystallography 61(7): 1009-1012 (2005)
AbstractEllipticine is a natural plant product that has been found to be a powerful anticancer drug. Although still unclear, its mechanism of action is considered to be mainly based on DNA intercalation and/or the inhibition of topoisomerase II. Many experimental data suggest an intercalation based on stacking interactions along the major base-pair axis, but alternative binding modes have been proposed, in particular for ellipticine derivatives. The 1.5 Å resolution structure of ellipticine complexed to a 6 bp oligonucleotide unveils its mode of binding and enables a detailed analysis of the distorting effects of the drug on the DNA. © 2005 International Union of Crystallography - all rights reserved.
Publisher version (URL)http://dx.doi.org/10.1107/S0907444905015404
Identifiersdoi: 10.1107/S0907444905015404
issn: 0907-4449
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