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Updated: Mar 8, 2026

Continuous Fluorescence-Based Endonuclease-Coupled DNA Methylation Assay to Screen for DNA Methyltransferase Inhibitors
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DNA Hypomethylating Drugs in Cancer Therapy

Takahiro Sato1, Jean-Pierre J Issa1,2, Patricia Kropf2

  • 1Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, Philadelphia, Pennsylvania 19140.

Cold Spring Harbor Perspectives in Medicine
|February 5, 2017
PubMed

Insights

Aberrant DNA methylation drives cancer by altering gene expression. DNA hypomethylating drugs reprogram cancer cells, enhancing sensitivity to chemotherapy and immunotherapy, offering a promising therapeutic strategy.

Area of Science:

  • Epigenetics and Cancer Biology
  • Pharmacology and Therapeutics

Background:

  • Aberrant DNA methylation is a hallmark of cancer, crucial for oncogene activation and tumor suppressor gene silencing.
  • DNA methylation alterations are key mechanisms by which cancer cells manipulate gene expression.
  • Targeting DNA methylation represents a significant strategy in cancer treatment.

Purpose of the Study:

  • To review preclinical and clinical data on DNA hypomethylating drugs for cancer therapy.
  • To highlight the role of DNA hypomethylating agents in reprogramming cancer cells.
  • To discuss the potential of these drugs in combination with chemotherapy and immunotherapy.

Main Methods:

  • Review of existing preclinical studies on DNA hypomethylating drugs.
  • Analysis of clinical trial data for hypomethylating agents in cancer treatment.
  • Examination of the impact of these drugs on cancer cell reprogramming and pathway modulation.

Main Results:

  • DNA hypomethylating drugs effectively reprogram tumor cells towards a more normal phenotype.
  • These drugs demonstrate significant potential in sensitizing cancer cells to chemotherapy and immunotherapy.
  • First-generation drugs (azacitidine, decitabine) are established treatments for myeloid leukemias; next-generation drugs are in development.

Conclusions:

  • DNA hypomethylating drugs are a viable and evolving therapeutic approach for various cancers.
  • Their ability to affect multiple pathways and enhance other treatments underscores their importance.
  • Further clinical investigation of next-generation hypomethylating agents is warranted.

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