Histone lysine demethylases as targets for anticancer therapy

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Jonas W Højfeldt1, Karl Agger, Kristian Helin

  • 11] Biotech Research and Innovation Centre (BRIC), University of Copenhagen, Ole Maaløes Vej 5, 2200 Copenhagen, Denmark. [2] Centre for Epigenetics, University of Copenhagen, Ole Maaløes Vej 5, 2200 Copenhagen, Denmark. [3].

Nature Reviews. Drug Discovery
|November 16, 2013
PubMed

Insights

Genes regulating epigenetic programs are implicated in human cancers, highlighting chromatin proteins as drug targets. Histone lysine demethylase inhibitors show promise for epigenetic cancer therapy.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Oncology

Background:

  • Genes controlling epigenetic programs are crucial for chromatin structure and cell identity.
  • Dysregulation of these genes contributes to human cancer development.
  • Epigenetic therapy, including DNA methylation and histone deacetylase (HDAC) inhibitors, is an emerging cancer treatment strategy.

Purpose of the Study:

  • To review key biological findings on the role of histone lysine demethylases in cancer.
  • To discuss the therapeutic potential and challenges of targeting these enzymes.
  • To highlight emerging small-molecule inhibitors for histone lysine demethylases.

Main Methods:

  • Literature review of biological findings.
  • Analysis of therapeutic strategies targeting histone lysine demethylases.
  • Overview of small-molecule inhibitor development.

Main Results:

  • Histone lysine demethylases play significant roles in various cancer types.
  • Targeting these enzymes presents both opportunities and challenges for cancer treatment.
  • Several small-molecule inhibitors targeting histone lysine demethylases are under development.

Conclusions:

  • Histone lysine demethylases are critical players in oncogenesis.
  • Targeting histone lysine demethylases offers a promising avenue for novel epigenetic cancer therapies.
  • Further research and development of specific inhibitors are essential for clinical translation.

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