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Updated: Mar 7, 2026

Extraction of Histones from Clinical Specimens for Epigenetic Profiling by Mass Spectrometry
Published on: November 21, 2025
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.
Abstract:
Reversible histone methylation has emerged in the last few years as an important mechanism of epigenetic regulation. Histone methyltransferases and demethylases have been identified as contributing factors in the development of several diseases, especially cancer. Therefore, they have been postulated to be new drug targets with high therapeutic potential. Here, we review histone demethylases with a special focus on their potential role in oncology drug discovery. We present an overview over the different classes of enzymes, their biochemistry, selected data on their role in physiology and already available inhibitors.
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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