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Targeting Histone Demethylases: A New Avenue for the Fight against Cancer

Dante Rotili1, Antonello Mai

  • 1Pasteur Institute-Cenci-Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Rome, Italy.

Genes & Cancer
|September 24, 2011
PubMed

Insights

Epigenetic alterations, specifically histone methylation, are implicated in cancer development. The discovery of histone Lys demethylases (KDMs) offers new diagnostic and therapeutic targets for cancer treatment.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Oncology

Background:

  • Epigenetic alterations, including histone modifications, play a role in cancer alongside genetic disorders.
  • Dysregulation of histone acetylation and methylation marks is linked to oncogenesis and tumor proliferation.
  • Histone methylation was historically viewed as stable, but recent discoveries reveal its dynamic nature.

Purpose of the Study:

  • To explore the role of dynamic histone methylation in biological processes.
  • To investigate histone Lys demethylases (KDMs) as potential diagnostic tools and therapeutic targets in cancer.
  • To present initial findings on modulating KDMs for novel cancer therapies.

Main Methods:

  • Review of recent discoveries concerning histone Lys demethylases (KDMs).
  • Analysis of the association between KDM alterations and various cancer types.
  • Exploration of the potential of KDMs as epigenetic targets.

Main Results:

  • The discovery of numerous histone Lys demethylases (KDMs) has revealed the dynamic nature of histone methylation.
  • Overexpression, alteration, or mutation of several KDMs is observed in diverse cancers.
  • KDMs are emerging as significant factors in oncogenesis and tumor proliferation.

Conclusions:

  • Dynamic histone methylation, regulated by KDMs, is crucial in biological processes.
  • KDMs represent promising diagnostic markers and therapeutic targets for cancer treatment.
  • Further research into KDMs could lead to novel epigenetic therapies against cancer.
Keywords:
2-oxoglutarateFADJumonji-containing enzymesLSD1cancer

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