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Bromodomain containing proteins PB1, SMARCA4, and SMARCA2 are important components of SWI/SNF chromatin remodeling complexes. We identified bromodomain inhibitors that target these proteins and display unusual binding modes involving water displacement from the KAc binding site. The best compound binds the fifth bromodomain of PB1 with a KD of 124 nM, SMARCA2B and SMARCA4 with KD values of 262 and 417 nM, respectively, and displays excellent selectivity over bromodomains other than PB1, SMARCA2, and SMARCA4.

Original publication

DOI

10.1021/acs.jmedchem.5b01997

Type

Journal article

Journal

J Med Chem

Publication Date

26/05/2016

Volume

59

Pages

5095 - 5101

Keywords

DNA Helicases, Dose-Response Relationship, Drug, Humans, Models, Molecular, Molecular Structure, Nuclear Proteins, Pyrroles, Quinazolinones, Structure-Activity Relationship, Transcription Factors