Ontology highlight
ABSTRACT:
SUBMITTER: Clark PG
PROVIDER: S-EPMC4449114 | biostudies-literature | 2015 May
REPOSITORIES: biostudies-literature
Clark Peter G K PG Vieira Lucas C C LC Tallant Cynthia C Fedorov Oleg O Singleton Dean C DC Rogers Catherine M CM Monteiro Octovia P OP Bennett James M JM Baronio Roberta R Müller Susanne S Daniels Danette L DL Méndez Jacqui J Knapp Stefan S Brennan Paul E PE Dixon Darren J DJ
Angewandte Chemie (International ed. in English) 20150413 21
The bromodomain-containing proteins BRD9 and BRD7 are part of the human SWI/SNF chromatin-remodeling complexes BAF and PBAF. To date, no selective inhibitor for BRD7/9 has been reported despite its potential value as a biological tool or as a lead for future therapeutics. The quinolone-fused lactam LP99 is now reported as the first potent and selective inhibitor of the BRD7 and BRD9 bromodomains. Development of LP99 from a fragment hit was expedited through balancing structure-based inhibitor de ...[more]