| Literature DB >> 18975896 |
Raphaël Rodriguez1, Sebastian Müller, Justin A Yeoman, Chantal Trentesaux, Jean-François Riou, Shankar Balasubramanian.
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.Entities:
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Year: 2008 PMID: 18975896 PMCID: PMC2746963 DOI: 10.1021/ja805615w
Source DB: PubMed Journal: J Am Chem Soc ISSN: 0002-7863 Impact factor: 15.419