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Updated: Dec 13, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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DNA Methyltransferases in Cancer: Biology, Paradox, Aberrations, and Targeted Therapy

Jiayu Zhang1,2, Cheng Yang1,2, Chunfu Wu1,2

  • 1Department of Pharmacology, Shenyang Pharmaceutical University, Shenyang 110016, China.

Cancers
|August 6, 2020
PubMed

Insights

DNA methyltransferases (DNMTs) are crucial epigenetic regulators involved in normal development and gene transcription. Aberrant DNMT functions are linked to cancer, but their precise role and therapeutic targeting remain complex and under investigation.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Cancer Biology

Background:

  • DNA methyltransferases (DNMTs) are key epigenetic modifiers regulating gene expression.
  • DNMTs (DNMT1, DNMT3A, DNMT3B) are vital for mammalian development, differentiation, and transcription.
  • Dysregulation of DNMTs is frequently implicated in tumorigenesis and cancer progression.

Purpose of the Study:

  • To summarize the biological functions and paradoxical roles of DNMTs in cancer.
  • To discuss emerging therapeutic strategies targeting DNMTs in tumors.
  • To provide novel insights for cancer therapy development.

Main Methods:

  • Literature review and synthesis of existing research on DNMTs in epigenetics and cancer.
  • Analysis of the dual roles of DNMTs in tumor suppression and promotion.
  • Exploration of current and novel therapeutic approaches targeting DNMTs.

Main Results:

  • DNMTs play complex roles in cancer, influencing tumor suppressor gene methylation and genomic instability.
  • Aberrant DNMT activity can increase tumor malignancy and negatively impact patient prognosis.
  • The precise impact of DNMTs on tumors is still debated, necessitating further research.

Conclusions:

  • DNMTs are critical epigenetic regulators with complex and sometimes contradictory roles in cancer.
  • Targeting DNMTs presents a promising but challenging avenue for cancer therapy.
  • Further investigation into DNMT functions and targeted therapies may yield novel treatment strategies.
Keywords:
DNA methyltransferasesDNMT aberrationscancertherapy

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