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Cyclometalated 1,3-bis(8-quinolyl) phenyl chloroplatinum(II) (Pt1) shows selective luminescence transduction of G-quadruplex binding over duplex DNA. The effect is enhanced on association with parallel and hybrid G-quadruplex structures over other topologies. The kinetics of binding are studied for c-myc and the response is found to be partially reversible in a displacement assay. Show less

G-quadruplexes turned out to be important targets for the development of novel targeted anticancer/antiviral therapies. More than 3000 G-quadruplex small-molecule ligands have been described, with most of them exerting anticancer/antiviral activity by inducing telomeric damage and/or altering oncogene or viral gene expression in cancer cells and viruses, respectively. For some ligands, in-depth NMR and/or crystallographic studies were performed, providing detailed knowledge on their interactions with diverse G-quadruplex targets. Here, the PDB-deposited NMR and crystal structures of the complexes between telomeric, oncogenic or viral G-quadruplexes and small-molecule ligands, of both organic and metal-organic nature, have been summarized and described based on the G-quadruplex target, from telomeric DNA and RNA G-quadruplexes to DNA oncogenic G-quadruplexes, and finally to RNA viral G-quadruplexes. An overview of the structural details of these complexes is here provided to guide the design of novel ligands targeting more efficiently and selectively cancer- and virus-related G-quadruplex structures. Platella, C.; Montesarchio, D. Insights into the Small Molecule Targeting of Show less