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DNA has been one of the privileged cellular target in cancer research since the understanding of the nitrogen mustard gas mode of action reported in 1946. Chemotherapeutics targeting DNA have proven to be extremely effective drugs and to constitute a major step forward in the survival of cancer patients. During the last decades, the pursuit for more selective anticancer agents has emulated the development of new drugs able to recognize non-canonical DNA
substructures that are found in cancer cells such as mismatches and G-quadruplexes (G4s). G4s, in which DNA assembles in the stacking of at least two guanine quartets, constitute a more and more studied target as they are well differentiated from duplex DNA. Furthermore, G4 DNA was reported to play a key role in the development of cancer being involved in the immortalisation process by virtue of their abundance in telomeric regions. G4 DNA appeared to be in higher prevalence in cancer cells, which has opened a new field for more targeted therapies.