Ontology highlight
ABSTRACT:
SUBMITTER: Drouin L
PROVIDER: S-EPMC4441536 | biostudies-literature | 2015 Mar
REPOSITORIES: biostudies-literature
Drouin Ludovic L McGrath Sally S Vidler Lewis R LR Chaikuad Apirat A Monteiro Octovia O Tallant Cynthia C Philpott Martin M Rogers Catherine C Fedorov Oleg O Liu Manjuan M Akhtar Wasim W Hayes Angela A Raynaud Florence F Müller Susanne S Knapp Stefan S Hoelder Swen S
Journal of medicinal chemistry 20150226 5
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 che ...[more]