There is currently significant interest in the development of G-quadruplex-interactive compounds, given the relationship between the ability to stabilize these non-canonical DNA structures and anticancer activity. In this study, a set of biophysical assays was applied to evaluate the binding of six drug-like ligands to DNA G-quadruplexes with different folding topologies. Interestingly, two of the investigated ligands showed selective G-quadruplex-stabilizing properties and biological activity. These compounds may represent useful leads for the development of more potent and selective ligands.

Looking for efficient G-quadruplex ligands: Evidence for selective stabilizing properties and telomere damage by drug-like molecules

PAGANO, BRUNO
Primo
;
AMATO, JUSSARA
Secondo
;
IACCARINO, NUNZIA;NOVELLINO, ETTORE;RANDAZZO, ANTONIO
Ultimo
2015

Abstract

There is currently significant interest in the development of G-quadruplex-interactive compounds, given the relationship between the ability to stabilize these non-canonical DNA structures and anticancer activity. In this study, a set of biophysical assays was applied to evaluate the binding of six drug-like ligands to DNA G-quadruplexes with different folding topologies. Interestingly, two of the investigated ligands showed selective G-quadruplex-stabilizing properties and biological activity. These compounds may represent useful leads for the development of more potent and selective ligands.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11588/604809
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