Monohydrazone Based G-Quadruplex Selective Ligands Induce DNA Damage and Genome Instability in Human Cancer Cells
Jussara Amato, Giulia Miglietta, Rita Morigi, Nunzia Iaccarino, Alessandra Locatelli, Alberto Leoni, Ettore Novellino, Bruno Pagano, Giovanni Capranico, Antonio Randazzo
Abstract
biophysical studies were performed employing both telomeric and oncogene promoter G-quadruplex-forming sequences. The obtained results allowed the identification of a highly selective G-quadruplex ligand that, when studied in human cancer cells, proved to be able to stabilize both G-quadruplexes and R loops and showed a potent cell killing activity associated with the formation of micronuclei, a clear sign of genome instability.
Topics & Concepts
G-quadruplexChemistryHuman genomeIn vitroCancer cellGenome instabilityDNACancerMicronucleus testLigand (biochemistry)OncogeneComputational biologyDNA damageGenomeCell biologyCellCancer researchBiochemistryGeneBiologyGeneticsCell cycleToxicityReceptorOrganic chemistryDNA and Nucleic Acid ChemistryAdvanced biosensing and bioanalysis techniquesRNA Interference and Gene Delivery