Published in
American Chemical Society, Journal of the American Chemical Society, 47(130), p. 15758-15759, 2008
DOI: 10.1021/ja805615w
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- American Chemical Society
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- [www.researchgate.net] | PDF
- [www.ncbi.nlm.nih.gov] | PDF
- [www.ncbi.nlm.nih.gov] | PDF
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A Novel Small Molecule That Alters Shelterin Integrity and Triggers a DNA-Damage Response at Telomeres
,
Justin A. Yeoman,
Chantal Trentesaux,
Jean-François Riou,
Shankar Balasubramanian
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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.