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Hitting histone demethylases [PDF]
Science-Business eXchange, 2012 A GSK–Structural Genomics Consortium team has identified the first potent and selective histone demethylase inhibitor and shown that the molecule dampens the macrophage inflammatory response. The pharma now is focusing on internal efforts and external approaches to exploring potential therapeutic applications of the inhibitor.
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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 +5 more
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Evolutionary history of histone demethylase families: distinct evolutionary patterns suggest functional divergence [PDF]
, 2008 Background Histone methylation can dramatically affect chromatin structure and gene expression and was considered irreversible until recent discoveries of two families of histone demethylases, the KDM1 (previously LSD1) and JmjC domain-containing ...
Xiaofan Zhou, Hong Ma
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Histone lysine demethylases in breast cancer [PDF]
Critical Reviews in Oncology/Hematology, 2013 Histone lysine demethylases (KDMs) have been recently discovered in mammals and have been nicknamed "erasers" for their ability to remove methyl groups from histone substrates. In cancer cells, KDMs can activate or repress gene transcription, behaving as oncogenes or tumor suppressors depending upon the cellular context.
PAOLICCHI, ELISA +4 more
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Targeting histone methyltransferases and demethylases in clinical trials for cancer therapy [PDF]
, 2016 Drawing of Object No ...
Ludovica Morera +2 more
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Systematic discovery of genetic modulation by Jumonji histone demethylases in Drosophila [PDF]
, 2017 Jumonji (JmjC) domain proteins influence gene expression and chromatin organization by way of histone demethylation, which provides a means to regulate the activity of genes across the genome.
Buszczak, Michael +6 more
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Histone demethylases in chromatin cross‐talks [PDF]
Biology of the Cell, 2011 The ‘histone code’ hypothesis states that chromatin‐based regulation of nuclear processes such as transcription is brought about by the combination of distinct modifications (histone marks) at specific loci. Its correct establishment involves chromatin cross‐talks, ensuring an ordered and concerted deposition/removal of a particular set of ...
Laure, Verrier +2 more
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JMJD3 is a histone H3K27 demethylase [PDF]
Cell Research, 2007 Histone methylation is an important epigenetic phenomenon that participates in a diverse array of cellular processes and has been found to be associated with cancer. Recent identification of several histone demethylases has proved that histone methylation is a reversible process.
Yang, Xiang +5 more
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KDM2 is a H3K4me3 demethylase regulating nucleolar organization [PDF]
, 2009 Background CG11033 (dKDM2) is the Drosophila homolog of the gene KDM2B. dKDM2 has been known to possess histone lysine demethylase activity towards H3K36me2 in cell lines and it regulates H2A ubiquitination.
Harsh H Kavi, James A Birchler
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Histone demethylase lysine demethylase 5B in development and cancer
Oncotarget, 2016 Histone methylation is one of the most important chromatin posttranslational modifications. It has a range of influences on nuclear functions including epigenetic inheritance, transcriptional regulation and the maintenance of genome integrity. Changes in histone methylation status take part in various physiological and pathological processes.
Han, Mengjiao +4 more
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