A structural analysis of G-quadruplex/ligand interactions

Haider, S.M., Neidle, S. and Parkinson, G.N. (2011) A structural analysis of G-quadruplex/ligand interactions. Biochimie, 93 (8). pp. 1239-1251. 10.1016/j.biochi.2011.05.012.

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DOI: 10.1016/j.biochi.2011.05.012

Abstract

This focused review article discusses in detail, all available high-resolution small molecule ligand/G-quadruplex structural data derived from crystallographic and NMR based techniques, in an attempt to understand key factors in ligand binding and to highlight the biological importance of these complexes. In contrast to duplex DNA, G-quadruplexes are four-stranded nucleic acid structures folded from guanine rich repeat sequences stabilized by the stacking of guanine G-quartets and extensive Watson-Crick/Hoogsteen hydrogen bonding. Thermally stable, these topologies can play a role in telomere regulation and gene expression. The core structures of G-quadruplexes form stable scaffolds while the loops have been shown, by the addition of small molecule ligands, to be sufficiently adaptable to generate new and extended binding platforms for ligands to associate, either by extending G-quartet surfaces or by forming additional planar dinucleotide pairings. Many of these structurally characterised loop rearrangements were totally unexpected opening up new opportunities for the design of selective ligands. However these rearrangements do significantly complicate attempts to rationally design ligands against well defined but unbound topologies, as seen for the series of napthalene diimides complexes. Drawing together previous findings and with the introduction of two new crystallographic quadruplex/ligand structures we aim to expand the understanding of possible structural adaptations available to quadruplexes in the presence of ligands, thereby aiding in the design of new selective entities.

Item Type:Article
Uncontrolled Keywords:G-quadruplex; Ligand binding; Structural analysis
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2732
Journal or Publication Title:Biochimie
Deposited By:Library Staff
Deposited On:20 Jan 2012 11:37
Last Modified:20 Jan 2012 11:37

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