The role of histone demethylases in cancer therapy

Inga Hoffmann1, Martin Roatsch, Martin L Schmitt

  • 1Institute of Pharmaceutical Sciences, Albert-Ludwigs-University of Freiburg, Albertstr. 25, 79104 Freiburg, Germany.

Molecular Oncology
|August 21, 2012
PubMed

Insights

Histone demethylases are key epigenetic regulators implicated in cancer. This review explores their role in oncology drug discovery, highlighting enzymes, biochemistry, and inhibitors.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Oncology

Background:

  • Reversible histone methylation is a critical epigenetic regulatory mechanism.
  • Histone methyltransferases and demethylases are implicated in disease development, particularly cancer.
  • These enzymes represent promising therapeutic targets for cancer treatment.

Purpose of the Study:

  • To review histone demethylases.
  • To focus on their potential in oncology drug discovery.
  • To provide an overview of enzyme classes, biochemistry, physiological roles, and inhibitors.

Main Methods:

  • Literature review of histone demethylases.
  • Analysis of enzyme classes and their biochemical properties.
  • Examination of physiological roles and existing inhibitors.

Main Results:

  • Histone demethylases are diverse enzyme classes.
  • Their dysregulation is linked to various cancers.
  • Several inhibitors targeting these enzymes are available or in development.

Conclusions:

  • Histone demethylases are significant targets for cancer drug discovery.
  • Further research into their inhibitors holds therapeutic promise.
  • Targeting epigenetic modifications offers a novel approach to cancer therapy.

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