The anticancer agent ellipticine unwinds DNA by intercalative binding in an orientation parallel to base pairs
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 stack...
| Autores: | , , , |
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| Tipo de recurso: | artículo |
| Fecha de publicación: | 2005 |
| País: | España |
| Institución: | Consejo Superior de Investigaciones Científicas (CSIC) |
| Repositorio: | DIGITAL.CSIC. Repositorio Institucional del CSIC |
| OAI Identifier: | oai:digital.csic.es:10261/108793 |
| Acceso en línea: | http://hdl.handle.net/10261/108793 |
| Access Level: | acceso abierto |
| Palabra clave: | Anticancer drugs intercalating agent ellipticine derivative ellipticine DNA Antineoplastic agents DNA binding drug design intercalators |
| Sumario: | 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 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. |
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