Lysine acetyltransferase 2B (KAT2B) (PCAF)

Lysine acetyltransferase 2B (KAT2B), widely known as p300/CBP-associated factor (PCAF), is a key epigenetic enzyme belonging to the Gcn5-related N-acetyltransferase (GNAT) family (UniProt P55201). It functions primarily by transferring an acetyl group from acetyl-CoA to the epsilon-amino group of lysine residues on histone H3 and H4, as well as various non-histone proteins like p53 and MyoD (PubMed: 22424615). This modification generally promotes an open chromatin state, facilitating active gene transcription and regulating processes such as the cell cycle, DNA repair, and cellular differentiation. PCAF is implicated in several pathologies; it acts as a co-activator for viral proteins like HIV-1 Tat, making it a target for anti-retroviral strategies, and shows dysregulation in multiple cancers including lung and colorectal carcinomas (PubMed: 28636116). Therapeutic strategies targeting PCAF include small-molecule inhibitors of its catalytic HAT domain and antagonists of its bromodomain, which are being explored for their potential to modulate aberrant gene expression in oncology and inflammatory diseases.

Other names

p300/CBP-associated factorHistone acetyltransferase PCAFP/CAFKAT2BGNAT family member

Inhibition of the catalytic histone acetyltransferase (HAT) domain to prevent protein acetylation, or competitive binding to the bromodomain to disrupt the recognition of acetylated lysine marks on chromatin (PubMed: 27153290).