A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1
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چکیده
منابع مشابه
A Cell-Permeable Ester Derivative of the JmjC Histone Demethylase Inhibitor IOX1
The 2-oxoglutarate (2OG)-dependent Jumonji C domain (JmjC) family is the largest family of histone lysine demethylases. There is interest in developing small-molecule probes that modulate JmjC activity to investigate their biological roles. 5-Carboxy-8-hydroxyquinoline (IOX1) is the most potent broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases, reported to date; howeve...
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The JmjC histone lysine demethylases (KDMs) are epigenetic regulators involved in the removal of methyl groups from post-translationally modified lysyl residues within histone tails, modulating gene transcription. These enzymes require molecular oxygen for catalytic activity and, as 2-oxoglutarate (2OG)-dependent oxygenases, are related to the cellular oxygen sensing HIF hydroxylases PHD2 and F...
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ژورنال
عنوان ژورنال: ChemMedChem
سال: 2014
ISSN: 1860-7179
DOI: 10.1002/cmdc.201300428