G-quadruplex (G4) and i-motif (iM) are four-stranded non-canonical nucleic acid structural arrangements. Recent evidences suggest that these DNA structures exist in living cells and could be involved in several cancer-related processes, thus representing an attractive target for anticancer drug discovery. Efforts toward the development of G4 targeting compounds have led to a number of effective bioactive ligands. Herein, employing several biophysical methodologies, we studied the ability of some well-known G4 ligands to interact with iM-forming DNA. The data showed that the investigated compounds are actually able to interact with both DNA in vitro, thus acting de facto as multi-target-directed agents. Interestingly, while all the compounds stabilize the G4, some of them significantly reduce the stability of the iM. The present study highlights the importance, when studying G4-targeting compounds, of evaluating also their behavior toward the i-motif counterpart.

Common G-quadruplex binding agents found to interact with i-motif-forming DNA: Unexpected multi-target-directed compounds / Pagano, Alessia; Iaccarino, Nunzia; Abdelhamid, Mahmoud A. S.; Brancaccio, Diego; Garzarella, Emanuele U.; Di Porzio, Anna; Novellino, Ettore; Waller, Zoë A. E.; Pagano, Bruno; Amato, Jussara; Randazzo, Antonio. - In: FRONTIERS IN CHEMISTRY. - ISSN 2296-2646. - 6:(2018), p. 281. [10.3389/fchem.2018.00281]

Common G-quadruplex binding agents found to interact with i-motif-forming DNA: Unexpected multi-target-directed compounds

Pagano, Alessia
Co-primo
;
Iaccarino, Nunzia
Co-primo
;
Brancaccio, Diego;Di Porzio, Anna;Novellino, Ettore;Pagano, Bruno;Amato, Jussara
Co-ultimo
;
Randazzo, Antonio
Co-ultimo
2018

Abstract

G-quadruplex (G4) and i-motif (iM) are four-stranded non-canonical nucleic acid structural arrangements. Recent evidences suggest that these DNA structures exist in living cells and could be involved in several cancer-related processes, thus representing an attractive target for anticancer drug discovery. Efforts toward the development of G4 targeting compounds have led to a number of effective bioactive ligands. Herein, employing several biophysical methodologies, we studied the ability of some well-known G4 ligands to interact with iM-forming DNA. The data showed that the investigated compounds are actually able to interact with both DNA in vitro, thus acting de facto as multi-target-directed agents. Interestingly, while all the compounds stabilize the G4, some of them significantly reduce the stability of the iM. The present study highlights the importance, when studying G4-targeting compounds, of evaluating also their behavior toward the i-motif counterpart.
2018
Common G-quadruplex binding agents found to interact with i-motif-forming DNA: Unexpected multi-target-directed compounds / Pagano, Alessia; Iaccarino, Nunzia; Abdelhamid, Mahmoud A. S.; Brancaccio, Diego; Garzarella, Emanuele U.; Di Porzio, Anna; Novellino, Ettore; Waller, Zoë A. E.; Pagano, Bruno; Amato, Jussara; Randazzo, Antonio. - In: FRONTIERS IN CHEMISTRY. - ISSN 2296-2646. - 6:(2018), p. 281. [10.3389/fchem.2018.00281]
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11588/722986
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