Discovery and Characterization of Small Molecule Inhibitors of Bromodomain Containing Proteins BRD9 and BRD7 – the Targetable Subunits of SWI/SNF Chromatin Remodeling Complexes
The Discovery of TG003 as the first dual non-BET (BRD9/7) BRD-kinase inhibitor.
VDW interactions deep inside the binding pocket of BRD7 significantly contributes to binding potency.
Potential steric clashes in BRD7 and induced fit binding mechanisms in BRD9 are the major determining factors for small
molecule inhibitors’ selectivity towards BRD9.