Related Experiment Video

Updated: Oct 11, 2025

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
06:07

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Published on: August 5, 2022

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Misregulation of the expression and activity of DNA methyltransferases in cancer

Isaiah K Mensah1, Allison B Norvil2, Lama AlAbdi3

  • 1Department of Biochemistry, Purdue University, West Lafayette, IN 47907, USA.

NAR Cancer
|December 6, 2021
PubMed

Insights

DNA methyltransferases (DNMTs) regulate DNA methylation. Aberrant DNMT activity and expression are hallmarks of cancer, driving uncontrolled cell proliferation and loss of identity.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Cancer Biology

Background:

  • DNA methyltransferases (DNMTs) are crucial for establishing and maintaining DNA methylation patterns in mammals.
  • DNMTs exhibit regional specificity through interactions with protein factors and chromatin modifications.
  • Altered DNMT expression or interactions lead to aberrant DNA methylation, a hallmark of cancer.

Purpose of the Study:

  • To review the structure, characteristics, and functions of DNMTs.
  • To examine the prevalence of DNMT mutations and abnormal expression in various cancers.
  • To explore factors mediating DNMT dysregulation and their impact on cancer development.

Main Methods:

  • Literature review focusing on DNMT structure, function, and cancer relevance.
  • Analysis of studies detailing DNMT mutations and expression patterns in cancer.
  • Synthesis of research on protein interactions and epigenetic modifications affecting DNMTs.

Main Results:

  • DNMTs (DNMT1, DNMT3A, DNMT3B, DNMT3L) play key roles in DNA methylation.
  • Aberrant DNA methylation (hyper- and hypomethylation) is prevalent in cancer, linked to increased cell proliferation and identity loss.
  • Somatic mutations in DNMTs are observed in cancers like Acute Myeloid Leukemia.
  • Existing DNMT inhibitors lack specificity, causing side effects.

Conclusions:

  • Understanding DNMT mechanisms is vital for cancer therapy.
  • Elucidating DNMTs' molecular roles can identify novel therapeutic targets.
  • Targeting DNMT complexes offers potential for more specific cancer treatments.

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