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; Amato, Jussara; Iaccarino, Nunzia; C., Cingolani; P., Zizza; A., Biroccio; Novellino, Ettore; Randazzo, Antonio. - In: CHEMMEDCHEM. - ISSN 1860-7179. - 10:4(2015), pp. 640-649. [10.1002/cmdc.201402552]
Looking for efficient G-quadruplex ligands: Evidence for selective stabilizing properties and telomere damage by drug-like molecules
PAGANO, BRUNOPrimo
;AMATO, JUSSARASecondo
;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.File | Dimensione | Formato | |
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