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Epigenetic Targets and their Inhibitors in Cancer Therapy

Le Zhao1,2, Yong-Tao Duan3, Ping Lu1

  • 1College of pharmacy, Henan University of Chinese Medicine, Zhengzhou, China.

Current Topics in Medicinal Chemistry
|December 25, 2018
PubMed

Insights

Epigenetic modifications, unlike genetic mutations, are reversible and offer new cancer treatment avenues. Research focuses on epigenetic drugs targeting DNA methylation and histone acetylation to restore normal cell function.

Area of Science:

  • Molecular Biology
  • Oncology
  • Pharmacology

Background:

  • Cancer development involves genetic mutations and epigenetic dysregulation.
  • Epigenetic mechanisms like DNA methylation and histone acetylation are crucial in cancer.
  • Epigenetic modifications are reversible, offering therapeutic potential.

Purpose of the Study:

  • To review the latest developments in epigenetic drugs for cancer therapy.
  • To discuss the application of epigenetic inhibitors in cancer treatment.

Main Methods:

  • Review of current epigenetic drugs and clinical trials.
  • Focus on inhibitors targeting DNA methylation and histone acetylation.
  • Exploration of novel epigenetic drug targets including BET proteins.

Main Results:

  • Approved epigenetic drugs primarily target DNA methylation and histone acetylation.
  • Numerous epigenetic drugs are in clinical trials targeting various epigenetic regulators.
  • Inhibitors of DNA methyltransferases, histone deacetylases, and BET proteins show promise.

Conclusions:

  • Epigenetic drugs represent a promising and reversible therapeutic strategy for cancer.
  • Targeting epigenetic modifications offers a new paradigm in cancer treatment.
  • Ongoing research and clinical trials are expanding the scope of epigenetic therapies.
Keywords:
CancerDNA methylationEpigenetic readersEpigenetics drugsHistone methylationHistones acetylationInhibitors.

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