Prospect of targeting lysine methyltransferase NSD3 for tumor therapy

Dan Li1, Tiantian Tian2, Chung-Nga Ko3

  • 1State Key Laboratory of Southwestern Chinese Medicine Resources, School of Pharmacy, Chengdu University of Traditional Chinese Medicine, Chengdu 610075, China.

PubMed

Insights

Nuclear receptor binding SET domain protein 3 (NSD3) is a key epigenetic target in cancer. Inhibiting NSD3 shows promise for developing new antitumor strategies by disrupting cancer cell growth and survival.

Area of Science:

  • Epigenetics
  • Cancer Biology
  • Molecular Oncology

Background:

  • Nuclear receptor binding SET domain protein 3 (NSD3) is increasingly recognized as a significant factor in oncogenesis.
  • NSD3 alterations (amplification, overexpression, mutation) are observed across various tumor types.
  • NSD3 plays a crucial role in regulating fundamental cellular processes including the cell cycle, apoptosis, DNA repair, and epithelial-mesenchymal transition (EMT).

Purpose of the Study:

  • To provide a comprehensive review of NSD3's structure and biological functions.
  • To highlight NSD3's role in promoting cancer development and progression.
  • To discuss the therapeutic potential of targeting NSD3, including inhibitors and degraders.

Main Methods:

  • Literature review and synthesis of existing research on NSD3.
  • Analysis of NSD3's involvement in key cancer-related pathways.
  • Review of current strategies for NSD3 inhibition and degradation.

Main Results:

  • NSD3 is implicated in promoting tumor development through its regulatory functions.
  • Targeting NSD3 (via inhibition, silencing, or knockdown) presents a promising avenue for cancer therapy.
  • The development of NSD3-specific inhibitors and degraders is an active area of research.

Conclusions:

  • NSD3 is a critical epigenetic regulator with significant oncogenic activity.
  • Targeting NSD3 offers a promising therapeutic strategy for various cancers.
  • Further development of NSD3-specific agents is warranted for effective cancer treatment.