Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

[Image: see text] Bromodomains are epigenetic reader domains that have recently become popular targets. In contrast to BET bromodomains, which have proven druggable, bromodomains from other regions of the phylogenetic tree have shallower pockets. We describe successful targeting of the challenging B...

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Detalhes bibliográficos
Main Authors: Ferguson, Fleur M., Fedorov, Oleg, Chaikuad, Apirat, Philpott, Martin, Muniz, Joao R. C., Felletar, Ildiko, von Delft, Frank, Heightman, Tom, Knapp, Stefan, Abell, Chris, Ciulli, Alessio
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2013
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3905694/
https://ncbi.nlm.nih.gov/pubmed/24304323
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm401582c
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