The role of NSD1, NSD2, and NSD3 histone methyltransferases in solid tumors

Iuliia Topchu, Rajendra P. Pangeni, Igor Bychkov, Sven A. Miller, Evgeny Izumchenko, Jindan Yu, Erica Golemis, John Karanicolas, Yanis Boumber*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

19 Scopus citations


NSD1, NSD2, and NSD3 constitute the nuclear receptor-binding SET Domain (NSD) family of histone 3 lysine 36 (H3K36) methyltransferases. These structurally similar enzymes mono- and di-methylate H3K36, which contribute to the maintenance of chromatin integrity and regulate the expression of genes that control cell division, apoptosis, DNA repair, and epithelial–mesenchymal transition (EMT). Aberrant expression or mutation of members of the NSD family is associated with developmental defects and the occurrence of some types of cancer. In this review, we discuss the effect of alterations in NSDs on cancer patient’s prognosis and response to treatment. We summarize the current understanding of the biological functions of NSD proteins, focusing on their activities and the role in the formation and progression in solid tumors biology, as well as how it depends on tumor etiologies. This review also discusses ongoing efforts to develop NSD inhibitors as a promising new class of cancer therapeutic agents.

Original languageEnglish (US)
Article number285
JournalCellular and Molecular Life Sciences
Issue number6
StatePublished - Jun 2022


  • Cancer
  • H3K36 methyltransferases
  • Histone methylation
  • NSD1/KMT3B
  • NSD3/WHSC1L1
  • Solid tumors

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Molecular Medicine
  • Molecular Biology
  • Cell Biology
  • Pharmacology


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