期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 130, 期 47, 页码 15758-+出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja805615w
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资金
- Cancer Research UK
- BBSRC
- Ligue Nationale Contre le Cancer
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 gamma H2AX foci colocalized at telomeres.
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