Selective inhibition of BET bromodomains

Epigenetic proteins are intently pursued targets in ligand discovery. To date, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic “writers” and “erasers”. Potent inhibitors of histone binding modules have not yet been described. Here we report a cell-permeab...

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Hlavní autoři: Filippakopoulos, Panagis, Qi, Jun, Picaud, Sarah, Shen, Yao, Smith, William B., Fedorov, Oleg, Morse, Elizabeth M., Keates, Tracey, Hickman, Tyler T., Felletar, Ildiko, Philpott, Martin, Munro, Shonagh, McKeown, Michael R., Wang, Yuchuan, Christie, Amanda L., West, Nathan, Cameron, Michael J., Schwartz, Brian, Heightman, Tom D., La Thangue, Nicholas, French, Christopher A., Wiest, Olaf, Kung, Andrew L., Knapp, Stefan, Bradner, James E.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2010
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Article
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC3010259/
https://ncbi.nlm.nih.gov/pubmed/20871596
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1038/nature09504
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