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Updated: Sep 5, 2025

In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing
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In Vitro Selection of Engineered Transcriptional Repressors for Targeted Epigenetic Silencing

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Diverse Functions of KDM5 in Cancer: Transcriptional Repressor or Activator?

Yasuyo Ohguchi1, Hiroto Ohguchi1

  • 1Division of Disease Epigenetics, Institute of Resource Development and Analysis, Kumamoto University, Kumamoto 860-0811, Japan.

Cancers
|July 9, 2022
PubMed

Insights

The KDM5 enzyme family, involved in epigenetic regulation, plays a dual role in gene transcription and is implicated in cancer development. Targeting KDM5 offers potential for novel cancer therapies by modulating chromatin remodeling.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Biochemistry

Background:

  • Epigenetic modifications, including histone post-translational modifications, are vital for gene expression and cellular function.
  • Enzymes like histone methyltransferases and demethylases regulate these modifications, and their dysregulation is linked to human diseases, particularly cancer.
  • The KDM5 family of enzymes specifically removes methyl groups from histone H3 lysine 4 (H3K4me2/3), a marker of active chromatin.

Purpose of the Study:

  • To review recent findings on the mechanisms of transcriptional regulation by KDM5 proteins.
  • To highlight the context-dependent roles of KDM5 as transcriptional repressors and activators.
  • To explore the therapeutic potential of targeting KDM5 in cancer treatment.

Main Methods:

  • Literature review of recent research on KDM5 family functions.
  • Analysis of KDM5-mediated transcriptional regulation in various cellular contexts.
  • Examination of KDM5's role in cancer pathogenesis and therapeutic strategies.

Main Results:

  • KDM5 proteins regulate the H3K4 methylation cycle, impacting active transcription.
  • KDM5 can act as both transcriptional repressors and activators, depending on the cellular context.
  • Dysregulation of KDM5 family members is frequently observed in various cancers.

Conclusions:

  • KDM5 proteins are key regulators of chromatin states and gene expression with significant implications in cancer.
  • Understanding the multifaceted roles of KDM5 is crucial for developing targeted cancer therapies.
  • Targeting KDM5 presents a promising avenue for future anti-cancer drug development.
Keywords:
KDM5MYCRNA polymerase IIcancerepigenetic regulatorhistone demethylase

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