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9H-Purine Scaffold Reveals Induced-Fit Pocket Plasticity of the BRD9 Bromodomain
[Image: see text] The 2-amine-9H-purine scaffold was identified as a weak bromodomain template and was developed via iterative structure based design into a potent nanomolar ligand for the bromodomain of human BRD9 with small residual micromolar affinity toward the bromodomain of BRD4. Binding of th...
Autores principales: | Picaud, Sarah, Strocchia, Maria, Terracciano, Stefania, Lauro, Gianluigi, Mendez, Jacqui, Daniels, Danette L., Riccio, Raffaele, Bifulco, Giuseppe, Bruno, Ines, Filippakopoulos, Panagis |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2015
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4403932/ https://www.ncbi.nlm.nih.gov/pubmed/25703523 http://dx.doi.org/10.1021/jm501893k |
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