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<title>Binding studies of metal–salphen and metal–bipyridine complexes towards G‐Quadruplex DNA</title>
<creator>Łęczkowska, Anna .</creator>
<creator>González García, Jorge .</creator>
<creator>Pérez Arnáiz, Cristina</creator>
<creator>García Ruiz, Begoña</creator>
<creator>White, Andrew J. P. .</creator>
<creator>Vilar, Ramón .</creator>
<subject>cancer</subject>
<subject>DNA binding</subject>
<subject>heterocycles</subject>
<subject>metal complexes</subject>
<subject>polymerase</subject>
<description>The proposed in vivo formation of G-quadruplex&#xd;
DNA (G4 DNA) in promoter regions of oncogenes and in telomeres&#xd;
has prompted the development of small molecules&#xd;
with high affinity and selectivity for these structures. Herein&#xd;
we report the synthesis of a new di-substituted bipyridine&#xd;
ligand and the corresponding complexes with Ni2+ and&#xd;
VO2+. Both these new complexes have been characterized&#xd;
spectroscopically and by X-ray crystallography. Detailed DNA&#xd;
binding studies of these two complexes, together with three&#xd;
previously reported metal salphen complexes, are presented.&#xd;
Using FRET melting assays, the binding affinity and selectivity&#xd;
of the five metal complexes against six different G4 DNA&#xd;
structures as well as a duplex DNA have been determined.&#xd;
In addition, we present detailed ITC and UV/Vis studies to&#xd;
characterize the interaction of the complexes with human&#xd;
telomeric G4 DNA. Finally, we show via a polymerase stop&#xd;
assay that these complexes are able to stabilize a G4 DNA&#xd;
structure (from the c-Myc oncogene promoter) and halt the&#xd;
activity of Taq polymerase.</description>
<date>2018-09-05</date>
<date>2019-08-09</date>
<date>2018-08</date>
<type>info:eu-repo/semantics/article</type>
<identifier>0947-6539</identifier>
<identifier>http://hdl.handle.net/10259/4911</identifier>
<identifier>10.1002/chem.201802248</identifier>
<language>eng</language>
<relation>Chemistry-a european journal. 2018, V. 24, n. 45, p. 11785-11794</relation>
<relation>https://doi.org/10.1002/chem.201802248</relation>
<relation>info:eu-repo/grantAgreement/EPSRC/EP/H005285/1</relation>
<rights>info:eu-repo/semantics/openAccess</rights>
<publisher>Wiley-VCH Verlag</publisher>
</thesis></metadata></record></GetRecord></OAI-PMH>