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...

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Detalles Bibliográficos
Autores principales: Picaud, Sarah, Strocchia, Maria, Terracciano, Stefania, Lauro, Gianluigi, Mendez, Jacqui, Daniels, Danette L., Riccio, Raffaele, Bifulco, Giuseppe, Bruno, Ines, Filippakopoulos, Panagis
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

Internet

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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