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

Bruno Pagano, Jussara Amato, Nunzia Iaccarino, Chiara Cingolani, Pasquale Zizza, Annamaria Biroccio, Ettore Novellino, Antonio Randazzo

Research output: Contribution to journalArticle

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.

Original languageEnglish
Pages (from-to)640-649
Number of pages10
JournalChemMedChem
Volume10
Issue number4
DOIs
Publication statusPublished - 2015

Keywords

  • anticancer agents
  • biological activity
  • DNA recognition
  • DNA structures
  • G-quadruplexes

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry
  • Molecular Medicine
  • Medicine(all)

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