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

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 BAZ2B bromodomain u...

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Veröffentlicht in:	Journal of medicinal chemistry 2013-12, Vol.56 (24), p.10183-10187
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Brief Drug Design Humans Ligands Models, Molecular Molecular Structure Proteins - antagonists & inhibitors Structure-Activity Relationship Transcription Factors, General Zinc Fingers - drug effects
Online-Zugang:	Volltext
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