Related Experiment Video

Updated: Mar 14, 2026

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

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Demethylating Agents in the Treatment of Cancer

Paul M Howell1, Zixing Liu2, Hung T Khong3

  • 1University of South Alabama, Mitchell Cancer Institute/1660 Springhill Ave., Mobile, AL 36604, USA. paulhowell@usouthal.edu.

Pharmaceuticals (Basel, Switzerland)
|October 8, 2016
PubMed

Insights

DNA methylation inhibitors, azacitidine and decitabine, are FDA-approved for myelodysplastic syndromes (MDS). This review covers their clinical data, benefits, toxicities, and use in solid tumors.

Area of Science:

  • Oncology
  • Epigenetics

Background:

  • Aberrant DNA methylation silences genes, promoting tumorigenesis.
  • DNA demethylating agents reactivate silenced genes in malignancies.

Approach:

  • Review of clinical data for azacitidine and decitabine.
  • Summary of clinical trials in myelodysplastic syndromes (MDS) and solid tumors.
  • Discussion of clinical benefits, toxicities, and limitations.

Key Points:

  • Azacitidine and decitabine are FDA-approved, standard-of-care treatments for MDS.
  • These demethylating agents have been investigated for solid tumor therapy.
  • Clinical benefits and toxicities are crucial considerations for their use.

Conclusions:

  • Azacitidine and decitabine show efficacy in MDS and are explored in solid tumors.
  • Understanding their limitations is key for optimizing cancer therapy.
  • Further research may refine the application of these epigenetic drugs.
Keywords:
azacitidinecancerdecitabineepigeneticsmethylation

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