Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

[Image: see text] The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodomain and extra terminal doma...

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Hauptverfasser: Hewings, David S., Fedorov, Oleg, Filippakopoulos, Panagis, Martin, Sarah, Picaud, Sarah, Tumber, Anthony, Wells, Christopher, Olcina, Monica M., Freeman, Katherine, Gill, Andrew, Ritchie, Alison J., Sheppard, David W., Russell, Angela J., Hammond, Ester M., Knapp, Stefan, Brennan, Paul E., Conway, Stuart J.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2013
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC3640414/
https://ncbi.nlm.nih.gov/pubmed/23517011
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm301588r
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