Epigenetic inhibitor silences KRAS-driven oncogenes

The methyltransferase NSD2 (MMSET) catalyses the histone modification H3K36me2 — a mark associated with active gene transcription — and is deregulated in various cancers, including those with KRAS mutations. A paper in Nature describes small-molecule NSD2 inhibitors that restore silent chromatin at oncogenes and show efficacy in aggressive KRAS-driven tumour models.

doi: https://doi.org/10.1038/d41573-025-00142-7