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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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Detalles Bibliográficos
Autores principales: 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: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2013
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3905694/
https://www.ncbi.nlm.nih.gov/pubmed/24304323
http://dx.doi.org/10.1021/jm401582c