title: Ruthenation of Non-stacked Guanines in DNA G-Quadruplex Structures: Enhancement of c-MYC Expression.
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.
authors.affiliation: Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), and Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
authors.forename: Jéssica
authors.initials: J
authors.lastname: Rodríguez
authors.affiliation: Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), and Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
authors.forename: Jesús
authors.initials: J
authors.lastname: Mosquera
authors.affiliation: Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), and Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
authors.forename: José R
authors.initials: JR
authors.lastname: Couceiro
authors.affiliation: Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), and Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
authors.forename: M Eugenio
authors.identifier: 0000-0001-7500-985X
authors.initials: ME
authors.lastname: Vázquez
authors.affiliation: Centro Singular de Investigación en Química Biolóxica e Materiais Moleculares (CIQUS), and Departamento de Química Orgánica, Universidade de Santiago de Compostela, 15782, Santiago de Compostela, Spain.
authors.forename: José L
authors.identifier: 0000-0002-7789-700X
authors.initials: JL
authors.lastname: Mascareñas
mesh_terms: D056831:Coordination Complexes / Q000737:chemistry / Q000494:pharmacology*; D004249:DNA Damage / Q000187:drug effects; D054856:G-Quadruplexes / Q000187:drug effects*; D016259:Genes, myc / Q000187:drug effects; D006147:Guanine / Q000737:chemistry; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D011401:Promoter Regions, Genetic / Q000187:drug effects*; D016271:Proto-Oncogene Proteins c-myc / Q000235:genetics*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry / Q000494:pharmacology*; D015854:Up-Regulation / Q000187:drug effects*
chemical_list: D056831:Coordination Complexes; C489427:MYC protein, human; D016271:Proto-Oncogene Proteins c-myc; D011725:Pyridines; D006147:Guanine; D012428:Ruthenium
keywords: DNA damage; bioinorganic chemistry; metalation; photochemistry; ruthenium