Structure‐Based Screening of Tetrazolylhydrazide Inhibitors versus KDM4 Histone Demethylases
نویسندگان
چکیده
منابع مشابه
KDM4/JMJD2 histone demethylases: epigenetic regulators in cancer cells.
Lysine methylation is one of the most prominent histone posttranslational modifications that regulate chromatin structure. Changes in histone lysine methylation status have been observed during cancer formation, which is thought to be a consequence of the dysregulation of histone lysine methyltransferases or the opposing demethylases. KDM4/JMJD2 proteins are demethylases that target histone H3 ...
متن کاملDrosophila Kdm4 demethylases in histone H3 lysine 9 demethylation and ecdysteroid signaling
The dynamic regulation of chromatin structure by histone post-translational modification is an essential regulatory mechanism that controls global gene transcription. The Kdm4 family of H3K9me2,3 and H3K36me2,3 dual specific histone demethylases has been implicated in development and tumorigenesis. Here we show that Drosophila Kdm4A and Kdm4B are together essential for mediating ecdysteroid hor...
متن کاملCORRIGENDUM: Drosophila Kdm4 demethylases in histone H3 lysine 9 demethylation and ecdysteroid signalling
The original version of this Article contained typographical errors in the spelling of the authors Pranabananda Dutta and Robin Shang, which were incorrectly given as Pranabanada Dutta and Robin Sheng, respectively. This has now been corrected in both the PDF and HTML versions of the Article.
متن کاملSelective Inhibitors of the JMJD2 Histone Demethylases: Combined Nondenaturing Mass Spectrometric Screening and Crystallographic Approaches†
Ferrous ion and 2-oxoglutarate (2OG) oxygenases catalyze the demethylation of N(epsilon)-methylated lysine residues in histones. Here we report studies on the inhibition of the JMJD2 subfamily of histone demethylases, employing binding analyses by nondenaturing mass spectrometry (MS), dynamic combinatorial chemistry coupled to MS, turnover assays, and crystallography. The results of initial bin...
متن کاملThe discovery of histone demethylases.
Histone methylation is a key element of the eukaryotic epigenome. Since the discovery of the first histone demethylase (HDM) in 2004, more than 20 demethylases have been identified and characterized. They belong to either the LSD family or the JmjC family, demonstrating the reversibility of all methylation states at almost all major histone lysine methylation sites. These findings ended decades...
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ژورنال
عنوان ژورنال: ChemMedChem
سال: 2019
ISSN: 1860-7179,1860-7187
DOI: 10.1002/cmdc.201900441