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Structure Enabled Design of BAZ2-ICR, a Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B

Structure Enabled Design of BAZ2-ICR, a Chemical Probe Targeting the Bromodomains of BAZ2A and BAZ2B

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, etc.

J Med Chem. 2015 Mar 12;58(5):2553-9.

PMID: 25719566

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR4242544	BAZ2-ICR			Price

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