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The Targeted Inhibition of Histone Lysine Demethylases as a Novel Promising Anti-Cancer Therapeutic Strategy-An

Jarosław Paluszczak1, Robert Kleszcz1

  • 1Department of Pharmaceutical Biochemistry, Poznan University of Medical Sciences, 60-806 Poznań, Poland.

Cancers
|September 13, 2025
PubMed

Insights

Histone lysine demethylases (KDMs) are key epigenetic regulators in cancer. Inhibiting KDMs shows significant anti-cancer potential, impacting cell growth and enhancing treatment sensitivity.

Area of Science:

  • Epigenetics
  • Oncology
  • Pharmacology

Background:

  • Non-mutational epigenetic reprogramming is a hallmark of cancer, driving tumor heterogeneity.
  • Histone lysine demethylases (KDMs) are epigenetic modulators frequently dysregulated in cancer.
  • KDM overexpression/hyperactivation contributes to cancer cell proliferation and survival.

Purpose of the Study:

  • To review recent evidence on the anti-cancer potential of KDM inhibitors.
  • To highlight KDMs as promising therapeutic targets in oncology.
  • To discuss the role of KDM inhibition in modulating cancer hallmarks.

Main Methods:

  • This review synthesizes current literature on KDM inhibitors in cancer.
  • Focuses on preclinical and clinical evidence of KDM inhibition.
  • Examines the impact of KDM inhibition on various cancer processes.

Main Results:

  • KDM inhibition affects cancer cell survival, proliferation, and motility.
  • Inhibiting specific KDMs like LSD1, KDM3, KDM4, KDM5, and KDM6 shows anti-cancer effects.
  • KDM inhibitors can enhance sensitivity to chemotherapy, radiation, and modulate anti-cancer immunity.

Conclusions:

  • KDM inhibitors represent a promising therapeutic strategy for cancer treatment.
  • Targeting KDMs offers a novel approach to combat cancer heterogeneity and plasticity.
  • Further research into KDM inhibitors could lead to improved cancer therapies.
Keywords:
KDMKDM4KDM5KDM6LSD1anti-cancer therapycancerepigeneticshistone lysine demethylases

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