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

✍ Scribed by Canals, Albert ;Purciolas, Mònica ;Aymamí, Joan ;Coll, Miquel


Book ID
104478111
Publisher
International Union of Crystallography
Year
2005
Tongue
English
Weight
664 KB
Volume
61
Category
Article
ISSN
0907-4449

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✦ Synopsis


Ellipticine 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 A 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.