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 mos Show more
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