Looking for Efficient G‐Quadruplex Ligands: Evidence for Selective Stabilizing Properties and Telomere Damage by Drug‐Like Molecules |
| |
Authors: | Dr Bruno Pagano Dr Jussara Amato Nunzia Iaccarino Dr Chiara Cingolani Dr Pasquale Zizza Dr Annamaria Biroccio Prof Ettore Novellino Prof Antonio Randazzo |
| |
Affiliation: | 1. Department of Pharmacy, University of Naples “Federico?II”, Via D. Montesano 49, 80131, Napoli (Italy);2. Experimental Chemotherapy Laboratory, Regina Elena National Cancer Institute, Via delle Messi d'Oro 156, 00158 Rome (Italy) |
| |
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. |
| |
Keywords: | anticancer agents biological activity DNA recognition DNA structures G‐quadruplexes |
|
|