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Synthèse et études d'Oligonucléotides et de Peptides comportant un Complexe Photoactivable de Ruthénium(II).

Abstract : The Ru(II) complexes have found widespread interest as luminescent DNA probes, or new phototherapeutic agent against cancer. Complexes containing highly π-deficient polyazaaromatic ligands such as TAP (1,4,5,8-tetraazaphenanthrene) under illumination are able to form specifically a photoadduct with the guanine nucleobase. This photoreactivity might be an extremely promising strategy to control the normal cellular process, and so perturb the gene expression. However, the lack of selectivity of this photoreaction blocks their therapeutic development.
To overcome this, we have realised the attachment of such metal complexes to the extremity of an oligonucleotide. This approach is based on the specific recognition of a target nucleotidic sequence by a nucleic acid probe. In this purpose, we have chosen to use the chemoselective oxime ligation. This coupling reaction was found to be highly efficient, between both unprotected moieties, with minimal chemical manipulation and working in physiological conditions. We have built some conjugate with two complexes of Ru(II) : [Ru(TAP)2Phen]2+ and [Ru(TAP)3]2+, anchoring at the 3' or 5' extremity of the oligonucléotides, in order to determine their photochemical potentiel. Then under visible illumination, we have demonstrated that the conjugates produce the specific and irreversible photocrosslinking between a guanine unit of the target and the ruthenium complex. Finally, we have also decided to extend our process by anchoring the complex [Ru(TAP)2Phen]2+ to cell-penetrating peptides.
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Contributor : Mathilde Villien <>
Submitted on : Tuesday, September 18, 2007 - 3:48:39 PM
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  • HAL Id : tel-00172987, version 1




Mathilde Villien. Synthèse et études d'Oligonucléotides et de Peptides comportant un Complexe Photoactivable de Ruthénium(II).. Autre. Université Joseph-Fourier - Grenoble I, 2007. Français. ⟨tel-00172987⟩



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