Covalent inhibition of NSD1 histone methyltransferase

August 31st, 2020 by Huang Huang

Nature Chemical Biology, Published online: 31 August 2020; doi:10.1038/s41589-020-0626-6

An irreversible small-molecule inhibitor of histone methyltransferase NSD1 is developed, which binds covalently to the C2062 residue in the catalytic SET domain and represses H3K36 dimethylation and target gene expression in leukemia cells.