Stabilization of G-quadruplex DNA by highly selective ligands via click chemistry.
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.
Moorhouse
Adam D
AD
Department of Pharmaceutical and Biological Chemistry, The School of Pharmacy, University of London, 29-39 Brunswick Square, London WC1N 1AX, United Kingdom.
Santos
Ana Mafalda
AM
Gunaratnam
Mekala
M
Moore
Michael
M
Neidle
Stephen
S
Moses
John E
JE
D004247:DNA / Q000737:chemistry* / Q000235:genetics; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D008024:Ligands; D008956:Models, Chemical; D015394:Molecular Structure; D013696:Temperature
D008024:Ligands; D004247:DNA