A Chemical Probe for the ATAD2 Bromodomain

ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF(2) as a sulfone bio-isostere to exploit the unique properties of f...

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Publicado en:Angew Chem Int Ed Engl
Main Authors: Bamborough, Paul, Chung, Chun-wa, Demont, Emmanuel H., Furze, Rebecca C., Bannister, Andrew J., Che, Ka Hing, Diallo, Hawa, Douault, Clement, Grandi, Paola, Kouzarides, Tony, Michon, Anne-Marie, Mitchell, Darren J., Prinjha, Rab K., Rau, Christina, Robson, Samuel, Sheppard, Robert J., Upton, Richard, Watson, Robert J.
Formato: Artigo
Idioma:Inglês
Publicado: 2016
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Article
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC7314595/
https://ncbi.nlm.nih.gov/pubmed/27530368
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1002/anie.201603928
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