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...

詳細記述

書誌詳細
主要な著者: Picaud, S, Strocchia, M, Terracciano, S, Lauro, G, Mendez, J, Daniels, D, Riccio, R, Bifulco, G, Bruno, I, Filippakopoulos, P
フォーマット: Journal article
言語:English
出版事項: American Chemical Society 2015