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  • RESEARCH HIGHLIGHT

Epigenetic inhibitor silences KRAS-driven oncogenes

By
  1. Alex Eccleston
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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.

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Nature Reviews Drug Discovery 24, 740 (2025)

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

References

  1. Jeong, J. et al. NSD2 inhibitors rewire chromatin to treat lung and pancreatic cancers. Nature https://doi.org/10.1038/s41586-025-09299-y (2025)

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