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Histone demethylases and their roles in cancer epigenetics

Alexandra D'Oto1, Qing-Wu Tian2, Andrew M Davidoff1

  • 1Department of Surgery, St Jude Children's Research Hospital, Memphis, USA.

Journal of Medical Oncology and Therapeutics
|February 3, 2017
PubMed

Insights

Cancer progression is linked to epigenetic changes like DNA methylation. This review covers human histone demethylases, their cancer roles, and new small molecule inhibitors for cancer therapy.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Oncology

Background:

  • Tumorigenesis involves genetic abnormalities and epigenetic alterations.
  • Histone modifications, including DNA methylation, are crucial in cancer development.
  • Histone demethylases are key regulators of the cancer epigenome.

Purpose of the Study:

  • To review human histone lysine demethylases and their functions in cancer.
  • To summarize recent advances in developing small molecule inhibitors targeting these enzymes for cancer treatment.

Main Methods:

  • Literature review of scientific publications.
  • Analysis of current knowledge on histone demethylases in cancer.
  • Overview of small molecule inhibitor development.

Main Results:

  • Histone demethylases play significant roles in cancer progression, metastasis, and therapy resistance.
  • Targeting histone demethylases with small molecule inhibitors shows therapeutic potential.

Conclusions:

  • Histone demethylases are critical players in cancer epigenetics.
  • Inhibitors targeting histone demethylases represent a promising avenue for novel cancer therapies.
Keywords:
CancerEpigeneticsHistone demethylase

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