A Novel Small Molecule That Alters Shelterin Integrity and Triggers a DNA-Damage Response at Telomeres
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- 31 October 2008
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 130 (47), 15758-15759
- https://doi.org/10.1021/ja805615w
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 γH2AX foci colocalized at telomeres.Keywords
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