title: Small-molecule quadruplex-targeted drug discovery.
abstract: Repeated guanine tracts in human and other genomes can form higher-order four stranded structures, termed quadruplexes. In the human genome they have particular prevalence in telomeric and promoter regions and also in 5'-UTRs and introns. These structures, if unresolved and stabilised by small molecules, can form impediments to transcription and translation, and thus can be considered as a form of gene targeting. This Digest surveys the major types of quadruplex-binding small molecules that have been designed and studied to date and directs attention to directions where future development of more drug-like compounds is likely to be most productive.
authors.affiliation: UCL School of Pharmacy, University College London, London WC1N 1AX, UK.
authors.forename: Stephan A
authors.initials: SA
authors.lastname: Ohnmacht
authors.affiliation: UCL School of Pharmacy, University College London, London WC1N 1AX, UK. Electronic address: s.neidle@ucl.ac.uk.
authors.forename: Stephen
authors.initials: S
authors.lastname: Neidle
mesh_terms: D018360:Crystallography, X-Ray; D016503:Drug Delivery Systems; D055808:Drug Discovery; D054856:G-Quadruplexes; D006801:Humans; D008958:Models, Molecular; D054852:Small Molecule Libraries
chemical_list: D054852:Small Molecule Libraries
keywords: Cancer; Quadruplex DNA, RNA; Small molecules