Bromodomain and PHD finger-containing protein 2 (BRPF2) (BRPF2)

Bromodomain and PHD finger-containing protein 2 (BRPF2), also known as BRD1, is a scaffold protein that plays a vital role in the assembly and activity of histone acetyltransferase (HAT) complexes, including MOZ/MORF and HBO1 [UniProt P55201]. The BRPF2 bromodomain specifically recognizes acetylated lysine residues, particularly H3K14ac, which allows it to direct HAT complexes to specific chromatin sites for gene activation [PubMed: 27105283]. This protein is essential for normal biological processes such as erythropoiesis and the maintenance of hematopoietic stem cells [PubMed: 22492969]. In clinical contexts, BRPF2 is implicated in the pathogenesis of various cancers and has been genetically linked to neurodevelopmental disorders like schizophrenia [PubMed: 28636011]. Therapeutic interest focuses on the BRPF2 bromodomain as a target for small-molecule inhibitors to modulate epigenetic signaling in disease [PubMed: 29182271]. Chemical probes like GSK6853 have been developed to selectively inhibit this domain, providing a foundation for potential drug development in oncology and neurology [PubMed: 29182271].

Other names

BRD1Bromodomain-containing protein 1BRPF1LBRPF2

Competitive inhibition of the bromodomain's acetyl-lysine binding pocket, preventing the recruitment of histone acetyltransferase complexes to chromatin.