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The Emerging Therapeutic Potential of Histone Methyltransferase and Demethylase Inhibitors

Authors

  • Astrid Spannhoff Dr.,

    1. Institute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstr. 25, 79104 Freiburg (Germany), Fax: (+49) 761036321
    2. The Virginia Harris Cockrell Cancer Research Center at The University of Texas, M.D. Anderson Cancer Center, 1808 Park Road 1C, Smithville, TX 78957 (USA)
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    • These authors contributed equally to this manuscript.

  • Alexander-Thomas Hauser,

    1. Institute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstr. 25, 79104 Freiburg (Germany), Fax: (+49) 761036321
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    • These authors contributed equally to this manuscript.

  • Ralf Heinke,

    1. Institute of Pharmacy, Martin-Luther Universität Halle-Wittenberg, Wolfgang-Langenbeckstr. 4, 06120 Halle (Saale) (Germany)
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  • Wolfgang Sippl Prof. Dr.,

    1. Institute of Pharmacy, Martin-Luther Universität Halle-Wittenberg, Wolfgang-Langenbeckstr. 4, 06120 Halle (Saale) (Germany)
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  • Manfred Jung Prof. Dr.

    1. Institute of Pharmaceutical Sciences, Albert-Ludwigs-Universität Freiburg, Albertstr. 25, 79104 Freiburg (Germany), Fax: (+49) 761036321
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Abstract

Epigenetics is defined as heritable changes to the transcriptome that are independent of changes in the genome. The biochemical modifications that govern epigenetics are DNA methylation and posttranslational histone modifications. Among the histone modifications, acetylation and deacetylation are well characterized, whereas the fields of histone methylation and especially demethylation are still in their infancy. This is particularly true with regard to drug discovery. There is strong evidence that these modifications play an important role in the maintenance of transcription as well as in the development of certain diseases. This article gives an overview of the mechanisms of action of histone methyltransferases and demethylases, their role in the formation of certain diseases, and available inhibitors. Special emphasis is placed on the strategies that led to the first inhibitors which are currently available and the screening approaches that were used in that process.

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