Histone acetyltransferase KAT2B (KAT2B)

Histone acetyltransferase KAT2B, commonly known as PCAF, is a critical epigenetic regulator that functions as both a histone acetyltransferase (HAT) and a transcriptional coactivator. The KAT2B bromodomain is a specialized protein module that recognizes and binds to acetylated lysine residues on histone tails, particularly H3K9 and H3K14, as well as non-histone proteins like p53 and HIV-1 Tat. This binding facilitates the assembly of multiprotein complexes required for gene activation and chromatin remodeling. In oncology, KAT2B is often dysregulated, acting as either an oncogene or a tumor suppressor depending on the cellular context, and is involved in the proliferation of various cancers including glioblastoma and lung cancer. Beyond cancer, the KAT2B bromodomain is a target of interest for its role in inflammatory signaling and viral replication, particularly in the context of HIV-1 latency. Small-molecule inhibitors targeting the KAT2B bromodomain aim to disrupt these epigenetic recognition events to modulate disease-associated gene expression profiles.

Other names

PCAFP300/CBP-associated factorK(lysine) acetyltransferase 2BLysine acetyltransferase 2B

Bromodomain inhibition (competitive binding to the acetyl-lysine recognition pocket to prevent protein-protein interactions and recruitment of transcriptional complexes)