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
It is now difficult to believe that a biological function for the left-handed Z-DNA and Z-RNA conformations was once controversial. The papers in this Special Issue, "Z-DNA and Z-RNA: from Physical St Show more
It is now difficult to believe that a biological function for the left-handed Z-DNA and Z-RNA conformations was once controversial. The papers in this Special Issue, "Z-DNA and Z-RNA: from Physical Structure to Biological Function", are based on presentations at the ABZ2021 meeting that was held virtually on 19 May 2021 and provide evidence for several biological functions of these structures. The first of its kind, this international conference gathered over 200 scientists from many disciplines to specifically address progress in research involving Z-DNA and Z-RNA. These high-energy left-handed conformers of B-DNA and A-RNA are associated with biological functions and disease outcomes, as evidenced from both mouse and human genetic studies. These alternative structures, referred to as "flipons", form under physiological conditions, regulate type I interferon responses and induce necroptosis during viral infection. They can also stimulate genetic instability, resulting in adaptive evolution and diseases such as cancer. The meeting featured cutting-edge science that was, for the most part, unpublished. We plan for the ABZ meeting to reconvene in 2022. Show less