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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.

Original publication

DOI

10.1021/jm501963e

Type

Journal article

Journal

Journal of medicinal chemistry

Publication Date

03/2015

Volume

58

Pages

2553 - 2559

Addresses

The Institute of Cancer Research, Division of Cancer Therapeutics, Cancer Research UK Cancer Therapeutics Unit , 15 Cotswold Road, Sutton, London SM2 5NG, U.K.

Keywords

Microsomes, Animals, Mice, Triazoles, Chromosomal Proteins, Non-Histone, Molecular Probes, Molecular Structure, Structure-Activity Relationship, Drug Design, Models, Molecular