Authors:
R Rodriguez, S Müller, JA Yeoman, C Trentesaux, J-F Riou, S Balasubramanian
Journal name: 
J Am Chem Soc
Citation info: 
130(47):15758-15759
Abstract: 
We describe a novel synthetic small molecule which shows an unprecedented stabilization of the human telomeric G-quadruplex with high selectivity relative to double-stranded DNA. We report that this compound can be used in vitro to inhibit telomerase activity and to uncap human POT1 (protection of telomeres 1) from the telomeric G-overhang. We also show that the small molecule G-quadruplex binder induces a partial alteration of shelterin through POT1 uncapping from telomeres in human HT1080 cancer cells and the presence of gammaH2AX foci colocalized at telomeres.
DOI: 
http://doi.org/10.1021/ja805615w
Research group: 
Balasubramanian Group
E-pub date: 
26 Nov 2008