Ruthenation of non-stacked guanines in DNA G-quadruplex structures : enhancement of c-MYC expression

Rodríguez, Jéssica and Mosquera, Jesús and Couceiro, José R. and Vázquez, M. Eugenio and Mascareñas, José L. (2016) Ruthenation of non-stacked guanines in DNA G-quadruplex structures : enhancement of c-MYC expression. Angewandte Chemie - International Edition, 55 (50). pp. 15615-15618. ISSN 1433-7851 (https://doi.org/10.1002/anie.201607965)

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Abstract

Guanine quadruplexes (GQs) are compact four-stranded DNA structures that play a key role in the control of a variety of biological processes, including gene transcription. Bulky ruthenium complexes featuring a bipyridine, a terpyridine, and one exchangeable ligand ([Ru(terpy)(bpy)X]n+) are able to metalate exposed guanines present in the GQ of the c-MYC promoter region that are not involved in quadruplex base pairing. qRT-PCR and western-blot experiments indicated that the complexes promote a remarkable increase in the expression of this oncogene. We also show that exchangeable thioether ligands (X=RSR′, Met) allow regulation of the metalating activity of the complex with visible light.

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