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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

Targeting DNA methylation for epigenetic therapy

Xiaojing Yang1, Fides Lay, Han Han

  • 1Department of Urology, Norris Comprehensive Cancer Center, Keck School of Medicine, University of Southern California, Los Angeles, CA, USA.

Trends in Pharmacological Sciences
|September 18, 2010
PubMed

Insights

DNA methylation patterns are crucial for development but disrupted in cancer, making them a therapeutic target. New hypomethylation agents show promise in treating cancers like myelodysplastic syndromes.

Area of Science:

  • Epigenetics
  • Cancer Biology
  • Pharmacology

Background:

  • DNA methylation patterns are established during development and copied during cell division.
  • The cancer epigenome, specifically the methylome, is significantly altered.
  • Epigenetic modifications are increasingly recognized as key players in cancer development.

Purpose of the Study:

  • To review the evolving understanding of the cancer epigenome.
  • To highlight the development and clinical application of DNA methylation-targeting drugs.
  • To discuss the latest cancer epigenetic models and hypomethylation agents.

Main Methods:

  • Review of current literature on DNA methylation and cancer epigenetics.
  • Analysis of drug development trends targeting DNA methylation.
  • Examination of clinical trial data for epigenetic therapies.

Main Results:

  • The cancer methylome is highly disrupted, presenting a viable target for therapies.
  • 5-Azacytidine is an effective epigenetic drug, recommended for high-risk myelodysplastic syndromes (MDS).
  • Numerous drugs targeting DNA methylation have been developed with improved efficacy and reduced toxicity.

Conclusions:

  • Epigenetic alterations in cancer are a significant area of research.
  • Hypomethylation agents represent a promising class of anticancer therapies.
  • Continued research into epigenetic modifications will drive the development of novel cancer treatments.

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