title: Stabilization of G-quadruplex DNA by highly selective ligands via click chemistry.
abstract: A series of G-quadruplex stabilizing compounds have been prepared via click chemistry employing the Cu(I)-catalyzed Huisgen reaction. These compounds were shown to bind tightly to G-quadruplex DNA even in the presence of competing high concentrations of duplex DNA. Furthermore, a modified TRAP assay has shown that some of these compounds also inhibit telomerase at low micromolar concentration.
authors.affiliation: Department of Pharmaceutical and Biological Chemistry, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
authors.forename: Adam D
authors.initials: AD
authors.lastname: Moorhouse
authors.forename: Ana Mafalda
authors.initials: AM
authors.lastname: Santos
authors.forename: Mekala
authors.initials: M
authors.lastname: Gunaratnam
authors.forename: Michael
authors.initials: M
authors.lastname: Moore
authors.forename: Stephen
authors.initials: S
authors.lastname: Neidle
authors.forename: John E
authors.initials: JE
authors.lastname: Moses
mesh_terms: D004247:DNA / Q000737:chemistry* / Q000235:genetics; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D008024:Ligands; D008956:Models, Chemical; D015394:Molecular Structure; D013696:Temperature
chemical_list: D008024:Ligands; D004247:DNA