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Targeting epigenetic regulators to overcome drug resistance in cancers

Nan Wang1, Ting Ma2, Bin Yu3

  • 1Institute of Drug Discovery & Development, School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou, 450001, China.

Signal Transduction and Targeted Therapy
|February 16, 2023
PubMed

Insights

Targeting epigenetic regulators, such as histone demethylases, can reverse cancer drug resistance. This review details their roles in tumor resistance and therapeutic strategies to overcome it.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Drug resistance leads to cancer recurrence and poor patient outcomes.
  • Epigenetic regulation, including DNA methylation and histone modification, influences gene expression without altering DNA sequence.
  • Aberrant epigenetic changes are increasingly linked to tumor drug resistance.

Purpose of the Study:

  • To review the role of epigenetic regulation in cancer drug resistance.
  • To comprehensively discuss the histone demethylase family and their mechanisms in cancer drug resistance.
  • To outline therapeutic strategies targeting histone demethylases to overcome drug resistance.

Main Methods:

  • Literature review focusing on epigenetic regulation and histone demethylases in cancer.
  • Analysis of studies detailing the functions of lysine-specific demethylase, Jumonji C-domain-containing demethylase, and histone arginine demethylase families.
  • Examination of therapeutic approaches including small-molecule inhibitors and small interfering RNA.

Main Results:

  • Epigenetic regulators, particularly histone demethylases, play crucial roles in the development of cancer drug resistance.
  • Specific histone demethylase families exhibit distinct regulatory mechanisms contributing to tumor resistance.
  • Targeting histone demethylases presents a promising strategy for reversing drug resistance.

Conclusions:

  • Epigenetic modifications are key drivers of cancer drug resistance.
  • Histone demethylases are critical targets for overcoming therapeutic challenges in oncology.
  • Therapeutic interventions aimed at histone demethylases offer potential to improve cancer treatment outcomes.

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