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...

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Veröffentlicht in:Journal of the American Chemical Society 2006-12, Vol.128 (50), p.15972-15973
Hauptverfasser: Moorhouse, Adam D, Santos, Ana Mafalda, Gunaratnam, Mekala, Moore, Michael, Neidle, Stephen, Moses, John E
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Sprache:eng
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Zusammenfassung: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.
ISSN:0002-7863
1520-5126
DOI:10.1021/ja0661919