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The bromodomain containing proteins BAZ2A/B play essential roles in chromatin remodeling and regulation of noncoding RNAs. We present the structure based discovery of a potent, selective, and cell active inhibitor 13 (BAZ2-ICR) of the BAZ2A/B bromodomains through rapid optimization of a weakly potent starting point. A key feature of the presented inhibitors is an intramolecular aromatic stacking interaction that efficiently occupies the shallow bromodomain pockets. 13 represents an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.

Citation

Ludovic Drouin, Sally McGrath, Lewis R Vidler, Apirat Chaikuad, Octovia Monteiro, Cynthia Tallant, Martin Philpott, Catherine Rogers, Oleg Fedorov, Manjuan Liu, Wasim Akhtar, Angela Hayes, Florence Raynaud, Susanne Müller, Stefan Knapp, Swen Hoelder. Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B. Journal of medicinal chemistry. 2015 Mar 12;58(5):2553-9

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PMID: 25719566

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