Nanosecond dynamics of G-quadruplex DNA in the presence of anticancer drugs.
G-rich DNA sequences are able to fold into structures called G-quadruplexes (G4). These structures are the focus of a number of studies in both fundamental and applied research, from cancer biology and novel therapeutics through to nanotechnology. Indeed, G4 motifs have been proposed to inhibit the reverse-transcriptase enzyme telomerase, which is up-regulated in over 85% of cancers but not in somatic cells. In recent years, there has been a growing interest in studying the G4s as attractive therapeutic targets for drugs like small molecule ligands that can stabilize their structure. In this context, nanosecond timescale motions are crucial because they give rise to the fast conformational rearrangements needed for the ligand to reach the high-affinity spot of the nucleic acid molecule. Here we propose to study how the binding of two anticancer drugs with different affinity, BRACO and Palmatin, affect the fast dynamics of G4s. The results could give novel insights, likely useful to formulate ligands more effective under the therapeutic point of view.
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Alessandro Paciaroni; COMEZ Lucia; valeria libera; LONGO Marialucia and SEYDEL Tilo. (2020). Nanosecond dynamics of G-quadruplex DNA in the presence of anticancer drugs.. Institut Laue-Langevin (ILL) doi:10.5291/ILL-DATA.8-04-880
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