Bromodomain-containing protein 2, Bromodomain-containing protein 3, Bromodomain-containing protein 4 (BRD2, BRD3, BRD4)

Bromodomain-containing protein 2 (BRD2), Bromodomain-containing protein 3 (BRD3), and Bromodomain-containing protein 4 (BRD4) are human proteins that belong to the BET family of epigenetic regulators, each featuring two tandem bromodomains and an extra-terminal domain which allow for selective binding to acetylated lysines on histones and non-histone proteins. These proteins act as transcriptional co-regulators, recruiting transcription factors, co-activators, or repressors, and are involved in cell cycle progression, gene expression regulation, chromatin structure maintenance, and the regulation of cell growth and differentiation. Aberrant function or overexpression of these proteins has been implicated in the pathogenesis of multiple malignancies (especially NUT midline carcinoma due to BRD4-NUT fusion), immune diseases, cardiovascular disorders, and metabolic dysfunctions. BET proteins are the targets for several classes of small-molecule inhibitors currently in clinical and preclinical development, most notably those characterized by mimicking acetyl-lysine to disrupt protein-protein interactions essential for oncogenic and inflammatory signaling.

Other names

RING3ORFXFSHRG2MCAP

Competitive inhibition of bromodomain interaction with acetylated lysines on histones and transcriptional regulators by mimicking acetyl-lysine and occupying the binding pocket; Downregulation of oncogene expression (e.g., MYC, cell cycle genes); Modulation of inflammatory and immune pathways