title: Looking for efficient G-quadruplex ligands: evidence for selective stabilizing properties and telomere damage by drug-like molecules.
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.
authors.affiliation: Department of Pharmacy, University of Naples "Federico II", Via D. Montesano 49, 80131, Napoli (Italy).
authors.forename: Bruno
authors.initials: B
authors.lastname: Pagano
authors.forename: Jussara
authors.initials: J
authors.lastname: Amato
authors.forename: Nunzia
authors.initials: N
authors.lastname: Iaccarino
authors.forename: Chiara
authors.initials: C
authors.lastname: Cingolani
authors.forename: Pasquale
authors.initials: P
authors.lastname: Zizza
authors.forename: Annamaria
authors.initials: A
authors.lastname: Biroccio
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Antonio
authors.initials: A
authors.lastname: Randazzo
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001483:Base Sequence; D002460:Cell Line; D004247:DNA / Q000737:chemistry; D015195:Drug Design; D054856:G-Quadruplexes / Q000187:drug effects*; D006801:Humans; D008024:Ligands; D062105:Molecular Docking Simulation; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D016615:Telomere / Q000737:chemistry / Q000187:drug effects*
chemical_list: D000970:Antineoplastic Agents; D008024:Ligands; D004247:DNA
keywords: DNA recognition; DNA structures; G-quadruplexes; anticancer agents; biological activity