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An Iridium(III) Complex Inhibits JMJD2 Activities and Acts as a Potential Epigenetic Modulator

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https://figshare.com/articles/dataset/An_Iridium_III_Complex_Inhibits_JMJD2_Activities_and_Acts_as_a_Potential_Epigenetic_Modulator/2136889
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A novel iridium­(III) complex was synthesized and evaluated for its ability to target JMJD2 enzymatic activity. The iridium­(III) complex 1 can inhibit JMJD2 activity and was selective for JMJD2 activity over JARID, JMJD3, and HDAC activities. Moreover, 1 suppressed the trimethylation of the p21 promoter on H3K9me3 and interrupted the JMJD2D–H3K9me3 interactions in human cells, suggesting that it could act as an epigenetic modulator. To our knowledge, 1 represents the first metal-based JMJD2 inhibitor reported in the literature.
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2016-02-13
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