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Ruthenation of Non‐stacked Guanines in DNA G‐Quadruplex Structures: Enhancement of c‐MYC Expression
Author(s) -
Rodríguez Jéssica,
Mosquera Jesús,
Couceiro José R.,
Vázquez M. Eugenio,
Mascareñas José L.
Publication year - 2016
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201607965
Subject(s) - chemistry , guanine , g quadruplex , terpyridine , dna , ruthenium , stereochemistry , ligand (biochemistry) , transcription (linguistics) , thioether , base pair , gene , metal , biochemistry , nucleotide , catalysis , receptor , linguistics , philosophy , organic chemistry
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.