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Recent Progress in Histone Demethylase Inhibitors
Journal of Medicinal Chemistry, 2016There 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 +6 more
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Histone demethylases in neurodevelopment and neurodegenerative diseases
International Journal of Neuroscience, 2023Neurodevelopment can be precisely regulated by epigenetic mechanisms, including DNA methylations, noncoding RNAs, and histone modifications. Histone methylation was a reversible modification, catalyzed by histone methyltransferases and demethylases. So far, dozens of histone lysine demethylases (KDMs) have been discovered, and they (members from KDM1 ...
Haiying, Wang +2 more
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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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The role of the histone demethylase KDM4A in cancer
Cancer Genetics, 2015Histone posttranslational modifications are important components of epigenetic regulation. One extensively studied modification is the methylation of lysine residues. These modifications were thought to be irreversible. However, several proteins with histone lysine demethylase functions have been discovered and characterized.
Lissania, Guerra-Calderas +4 more
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Interfering with histone demethylases in HSCs
Blood, 2013In this issue of Blood , Cellot et al identify the histone demethylase Jarid1b as a key regulator of renewal and differentiation in hematopoietic stem cells (HSCs).[1][1] ![Figure][2] Proposed model for JARID1B activity in HSC regulation.
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Histone lysine demethylases and their functions in cancer
International Journal of Cancer, 2020AbstractHistone lysine demethylases (KDMs) are enzymes that remove the methylation marks on lysines in nucleosomes' histone tails. These changes in methylation marks regulate gene transcription during both development and malignant transformation. Depending on which lysine residue is targeted, the effect of a given KDM on gene transcription can be ...
Jayden Sterling +3 more
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[Advances in histone methyltransferases and histone demethylases].
Ai zheng = Aizheng = Chinese journal of cancer, 2010Histone modification as one of the key epigenetic regulation mechanisms plays critical roles in various biological processes, including regulation of chromatin structure dynamics and gene expression. Both histone methyltransferase and histone demethylases contribute to the establishment and maintenance of different histone methylation status.
Xi, Wang, Wei-Guo, Zhu
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Histone demethylases and cancer.
Advances in cancer research, 2009Epigenetic modifications are heritable chromatin alterations that contribute to the temporal and spatial interpretation of the genome. The epigenetic information is conveyed through a multitude of chemical modifications, including DNA methylation, reversible modifications of histones, and ATP-dependent nucleosomal remodeling.
Sotirios C, Kampranis +1 more
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Drug discovery of histone lysine demethylases (KDMs) inhibitors (progress from 2018 to present)
European Journal of Medicinal Chemistry, 2022Hang Zhang, Yingqian Zhang
exaly