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    Por favor, use este identificador para citar o enlazar este ítem: http://hdl.handle.net/10259/4911

    Título
    Binding studies of metal–salphen and metal–bipyridine complexes towards G‐Quadruplex DNA
    Autor
    Łęczkowska, Anna .
    González García, Jorge .
    Pérez Arnáiz, CristinaAutoridad UBU Orcid
    García Ruiz, BegoñaAutoridad UBU Orcid
    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
    2018-08
    ISSN
    0947-6539
    DOI
    10.1002/chem.201802248
    Resumo
    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
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    Łe˛czkowska-chemistry_2018.pdf
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