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Título : Binding studies of metal–salphen and metal–bipyridine complexes towards G‐Quadruplex DNA
Autor : Łęczkowska, Anna .
González García, Jorge .
Pérez Arnáiz, Cristina
García Ruiz, Begoña
White, Andrew J. P. .
Vilar, Ramón .
Publicado en: Chemistry-a european journal. 2018, V. 24, n. 45, p. 11785-11794
Editorial : Wiley-VCH Verlag
Fecha de publicación : ago-2018
Fecha de disponibilidad: 9-ago-2019
ISSN : 0947-6539
DOI: 10.1002/chem.201802248
Resumen : The proposed in vivo formation of G-quadruplex DNA (G4 DNA) in promoter regions of oncogenes and in telomeres has prompted the development of small molecules with high affinity and selectivity for these structures. Herein we report the synthesis of a new di-substituted bipyridine ligand and the corresponding complexes with Ni2+ and VO2+. Both these new complexes have been characterized spectroscopically and by X-ray crystallography. Detailed DNA binding studies of these two complexes, together with three previously reported metal salphen complexes, are presented. Using FRET melting assays, the binding affinity and selectivity of the five metal complexes against six different G4 DNA structures as well as a duplex DNA have been determined. In addition, we present detailed ITC and UV/Vis studies to characterize the interaction of the complexes with human telomeric G4 DNA. Finally, we show via a polymerase stop assay that these complexes are able to stabilize a G4 DNA structure (from the c-Myc oncogene promoter) and halt the activity of Taq polymerase.
Palabras clave: cancer
DNA binding
heterocycles
metal complexes
polymerase
Materia: Química física
Chemistry, Physical and theoretical
URI : http://hdl.handle.net/10259/4911
Versión del editor: https://doi.org/10.1002/chem.201802248
Aparece en las colecciones: Artículos TERMOCIN

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