Results 201 to 210 of about 29,619 (246)

The KDM6 histone demethylase inhibitor GSK-J4 induces metal and stress responses in multiple myeloma cells

Cribbs AP, Hookway ES, Yapp C, Che K, Dunford JE, Gutheridge K, Lari F, Wells G, Philpott M, Cain P, Brotherton D, Palmer C, Maret W, Fitzgibbons J, Christianson JC, Oppermann U.   +15 more
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Inhibitors of histone demethylases

Bioorganic & Medicinal Chemistry, 2011
Methylated 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, Kristensen, Jesper L, Kristensen, Line H, Agger, Karl, Helin, Kristian, Gajhede, Michael, Clausen, Rasmus P   +6 more
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Histone demethylases in development and disease

Trends in Cell Biology, 2010
Histone modifications serve as regulatory marks that are instrumental for the control of transcription and chromatin architecture. Strict regulation of gene expression patterns is crucial during development and differentiation, where diverse cell types evolve from common predecessors. Since the first histone lysine demethylase was discovered in 2004, a
Pedersen, Marianne Terndrup, Helin, Kristian   +1 more
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The emerging functions of histone demethylases

Current Opinion in Genetics & Development, 2008
Epigenetic 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, Christensen, Jesper, Cloos, Paul Ac, Helin, Kristian   +3 more
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JMJD6 Is a Histone Arginine Demethylase

Science, 2007
Arginine 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, Yue, Chen, Yingming, Zhao, Richard K, Bruick   +3 more
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In Vitro Histone Demethylase Assays

2009
Histone 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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In Vitro Histone Demethylase Assays

2022
Dynamic 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

2015
Histone 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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Recent Progress in Histone Demethylase Inhibitors

Journal of Medicinal Chemistry, 2016
There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with small molecules both for the generation of probes for target exploration and for therapeutic purposes. Here we update on previous reviews on the inhibition of the lysine-specific demethylases (LSDs or KDM1s) and JmjC families of N-methyl-lysine demethylases (JmjC
McAllister, Tom E.; England, Katherine S.; Hopkinson, Richard J.; Brennan, Paul E.; Kawamura, Akane; Schofield, Christopher J.   +6 more
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Histone Demethylases

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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