Screening for Inhibitors of BRD4 Bromodomain Using a Homogeneous Proximity Assay

The BET family of proteins, which contain tandem repeats of Bromodomains plus an Extra Terminal domain, play a role in bridging acetylation and transcriptional regulation of diverse cellular processes such as inflammatory gene expression, mitosis and viral/host interactions. Several small molecule inhibitors have been identified that disrupt bromodomain/acetylated lysine interactions. In this application note from BioTek, the automation of a homogeneous TR-FRET assay method suitable for high throughput screening and rapid characterization of inhibitors of bromodomain/acetylated peptide interactions is described.