9H-purine scaffold reveals induced-fit pocket plasticity of the BRD9 bromodomain

The 2-amine-9<em>H</em>-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...

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Main Authors: Picaud, S, Strocchia, M, Terracciano, S, Lauro, G, Mendez, J, Daniels, D, Riccio, R, Bifulco, G, Bruno, I, Filippakopoulos, P
格式: Journal article
语言:English
出版: American Chemical Society 2015