Acta Crystallogr D Biol Crystallogr. 2005 Jul;61(Pt 7):1009-12. Epub 2005 Jun 24.

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

Canals A, Purciolas M, Aymamí J, Coll M.

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Institut de Biologia Molecular de Barcelona, Consejo Superior de Investigaciones Científicas, Parc Científic de Barcelona, Baldiri Reixac 10-12, 08028 Barcelona, Spain. acpcri@ibmb.csic.es

Abstract

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.

PMID:: 15983425; [PubMed - indexed for MEDLINE]

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Probing intercalation and conformational effects of the anticancer drug 2-methyl-9-hydroxyellipticinium acetate in DNA fragments with circular dichroism. [Eur J Biochem. 1992]
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Cited by 1 PubMed Central article

Molecular recognition of poly(A) by small ligands: an alternative method of analysis reveals nanomolar, cooperative and shape-selective binding. [Nucleic Acids Res. 2009]
Molecular recognition of poly(A) by small ligands: an alternative method of analysis reveals nanomolar, cooperative and shape-selective binding.
Cetinkol OP, Hud NV. Nucleic Acids Res. 2009 Feb; 37(2):611-21. Epub 2008 Dec 10.

Structures reported by this article

Structure Of Ellipticine In Complex With A 6-Bp Dna

PDB: 1Z3F

Source:

Method: X-Ray Diffraction

Resolution: 1.5 Å

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