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• W2790490201 abstract "Plant homeodomain (PHD) containing proteins are important epigenetic regulators and are of interest as potential drug targets. Inspired by the amiodarone derivatives reported to inhibit the PHD finger 3 of KDM5A (KDM5A(PHD3)), a set of compounds were synthesised. Amiodarone and its derivatives were observed to weakly disrupt the interactions of a histone H3K4me3 peptide with KDM5A(PHD3). Selected amiodarone derivatives inhibited catalysis of KDM5A, but in a PHD-finger independent manner. Amiodarone derivatives also bind to H3K4me3-binding PHD-fingers from the KDM7 subfamily. Further work is required to develop potent and selective PHD finger inhibitors." @default.
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• W2790490201 date "2018-07-01" @default.
• W2790490201 modified "2023-10-18" @default.
• W2790490201 title "Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases" @default.
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• W2790490201 doi "https://doi.org/10.1016/j.bmc.2018.03.030" @default.
• W2790490201 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6380468" @default.
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