Quadruplex DNA crystal structures and drug design.
Crystallographic studies of G-quadruplex nucleic acids have resulted in a small group of structures to date. Their morphological and detailed conformational features are described here, emphasizing the stability of the G-tetrad core and the flexibility of loops, especially upon ligand binding. Implications for drug design are discussed, in the context of the druggability of both telomeric and non-telomeric quadruplex DNAs.
Neidle
Stephen
S
The Cancer Research UK Biomolecular Structure Group, The School of Pharmacy, University of London, 29-39 Brunswick Square, London, WC1N 1AX, UK. stephen.neidle@pharmacy.ac.uk
Parkinson
Gary N
GN
D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry* / Q000378:metabolism; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D054856:G-Quadruplexes; D006801:Humans; D019098:Telomerase / Q000037:antagonists & inhibitors / Q000378:metabolism
D004791:Enzyme Inhibitors; D004247:DNA; D019098:Telomerase