The role of histone demethylases in cancer therapy |
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Authors: | Inga Hoffmann Martin Roatsch Martin L Schmitt Luca Carlino Martin Pippel Wolfgang Sippl Manfred Jung |
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Institution: | 1. Institute of Pharmaceutical Sciences, Albert-Ludwigs-University of Freiburg, Albertstr. 25, 79104 Freiburg, Germany;2. Department of Pharmaceutical Chemistry, Martin-Luther-University of Halle-Wittenberg, Germany |
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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. |
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Keywords: | Epigenetics Histone demethylases LSD1 JMJC Lysine demethylase |
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