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Inhibitors of histone demethylases
Bioorganic & Medicinal Chemistry, 2011Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared.
Lohse, Brian +6 more
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Lysine demethylases and cancer
Pathology - Research and PracticeEpigenetic mechanisms are of pivotal importance in the normal development and maintenance of cell and tissue-specific gene expression patterns, and are fundamental to the genesis of cancer. One significant category of epigenetic modifications is histone methylation.
Tomas, Eckschlager +2 more
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Histone Demethylases in Cancer [PDF]
Current Pharmacology Reports, 2015 Epigenetic regulation, which involves with covalent modifications of DNA and the protein that bundles DNA, namely histones, is an exciting and variable phenomenon that affects normal cellular genetic character and contributes to human diseases. One key histone modification is methylation, regulated by methyl transferases and demethylases.
Satheesh Sainathan +2 more
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In Vitro Histone Demethylase Assays
2009Histone methylation plays important roles in chromatin structure, transcription, and epigenetic state of the cell. Tremendous discoveries recently demonstrated that methylation mark is not static but is dynamically regulated by both histone methyltransferases and the histone demethylases.
Kenji, Kokura, Jia, Fang
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The emerging functions of histone demethylases
Current Opinion in Genetics & Development, 2008Epigenetic information refers to heritable changes in gene function that are stable between cell divisions but which is not a result of changes in the DNA sequence. Part of the epigenetic mechanism has been ascribed to modifications of histones or DNA that affects the transcription of specific genes. In this context, post-translational modifications of
Agger, Karl +3 more
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JMJD6 Is a Histone Arginine Demethylase
Science, 2007Arginine methylation occurs on a number of proteins involved in a variety of cellular functions. Histone tails are known to be mono- and dimethylated on multiple arginine residues where they influence chromatin remodeling and gene expression. To date, no enzyme has been shown to reverse these regulatory modifications.
Bingsheng, Chang +3 more
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In Vitro Histone Demethylase Assays
2022Dynamic histone methylation regulates gene activation and repression. It is involved in proliferation, differentiation, lineage specification, and development. Histone demethylase assays are invaluable in studying histone demethylation substrate recognition, kinetics, regulation, and inhibition by small molecules, many of which are potential ...
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In Vitro Histone Demethylase Assays
2015Histone methylation plays pivotal roles in modulating chromatin structure and dynamics and in turn regulates genomic processes that require access to the DNA template. The methylation status at different sites is dynamically regulated by histone methyltransferases and demethylases. During the past decade, two classes of proteins have been characterized
Kenji, Kokura, Lidong, Sun, Jia, Fang
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Histone methylation is a dynamic process that contributes to the control of gene expression by influencing chromatin structure. Since their initial discovery 20 years ago, histone demethylases have been shown to play a critical role in histone methylation and thus developmental, physiological, and pathological processes.
Stephen C. Kales, Anton Simeonov
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Stephen C. Kales, Anton Simeonov
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