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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.
The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs.,Canals A, Purciolas M, Aymami J, Coll M Acta Crystallogr D Biol Crystallogr. 2005 Jul;61(Pt 7):1009-12. Epub 2005, Jun 24. PMID:15983425[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
↑ Canals A, Purciolas M, Aymami J, Coll M. The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs. Acta Crystallogr D Biol Crystallogr. 2005 Jul;61(Pt 7):1009-12. Epub 2005, Jun 24. PMID:15983425 doi:S0907444905015404