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Looking for Efficient G‐Quadruplex Ligands: Evidence for Selective Stabilizing Properties and Telomere Damage by Drug‐Like Molecules
Author(s) -
Pagano Bruno,
Amato Jussara,
Iaccarino Nunzia,
Cingolani Chiara,
Zizza Pasquale,
Biroccio Annamaria,
Novellino Ettore,
Randazzo Antonio
Publication year - 2015
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201402552
Subject(s) - g quadruplex , telomere , chemistry , dna , folding (dsp implementation) , combinatorial chemistry , drug , molecule , computational biology , small molecule , drug discovery , stereochemistry , biophysics , biochemistry , biology , pharmacology , organic chemistry , electrical engineering , engineering
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.