Screening for histone codebreakers.

The lysine methyltransferase NSD2 is overexpressed and carries gain-of-function mutations in a number of different cancers, making it an attractive therapeutic target. However, no specific small molecule inhibitors have been identified for this enzyme, responsible for depositing the H3K36me2 mark on histones. A new study reports a robust platform for high-throughput screening (HTS) assays to facilitate this discovery.