A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases |
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| Authors: | Luo Xuelai Liu Yongxiang Kubicek Stefan Myllyharju Johanna Tumber Anthony Ng Stanley Che Ka Hing Podoll Jessica Heightman Tom D Oppermann Udo Schreiber Stuart L Wang Xiang |
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| Affiliation: | Department of Chemistry and Biochemistry, University of Colorado, Boulder, Colorado 80309, USA. |
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| Abstract: | Histone methylations are important chromatin marks that regulate gene expression, genomic stability, DNA repair, and genomic imprinting. Histone demethylases are the most recent family of histone-modifying enzymes discovered. Here, we report the characterization of a small-molecule inhibitor of Jumonji C domain-containing histone demethylases. The inhibitor derives from a structure-based design and preferentially inhibits the subfamily of trimethyl lysine demethylases. Its methyl ester prodrug, methylstat, selectively inhibits Jumonji C domain-containing his-tone demethylases in cells and may be a useful small-molecule probe of chromatin and its role in epigenetics. |
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