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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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2013
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3640414/
https://www.ncbi.nlm.nih.gov/pubmed/23517011
http://dx.doi.org/10.1021/jm301588r

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