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首页> 外文期刊>Journal of the American Chemical Society >A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases
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A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases

机译：包含Jumonji C结构域组蛋白去甲基化酶的细胞功能的选择性抑制剂和探针。

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摘要

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 histone demethylases in cells and may be a useful small-molecule probe of chromatin and its role in epigenetics.
机译：组蛋白甲基化是重要的染色质标记，可调节基因表达，基因组稳定性，DNA修复和基因组印迹。组蛋白脱甲基酶是最近发现的组蛋白修饰酶家族。在这里，我们报告含有Jumonji C域的组蛋白去甲基化酶的小分子抑制剂的表征。该抑制剂源自基于结构的设计，并优先抑制三甲基赖氨酸脱甲基酶的亚家族。它的甲酯前药即甲基稳定剂，选择性抑制细胞中含有Jumonji C结构域的组蛋白脱甲基酶，并且可能是染色质及其在表观遗传学中有用的小分子探针。

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  • 来源
    《Journal of the American Chemical Society》 |2011年第24期|p.9451-9456|共6页
  • 作者

    Xuelai Luo; Yongxiang Liu; Stefan Kubicek; Johanna Myllyharju; Anthony lumber; Stanley Ng; Ka Hing Che; Jessica Podoll; Tom D. Heightman; Udo Oppermann; Stuart L. Schreiber; Xiang Wang;

  • 作者单位

    Department of Chemistry and Biochemistry, University of Colorado, Boulder, Colorado 80309, United States,Department of Surgery, Tongji Hospital, Huazhong University of Sdence and Technology, 1095 Jiefang Road, Wuhan, Hubei,430030, People's Republic of China.;

    Department of Chemistry and Biochemistry, University of Colorado, Boulder, Colorado 80309, United States;

    The Howard Hughes Medical Institute at the Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, Massachusetts02142, United States,Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, United States,CeMM — Research Center for Molecular Medicine of the Austrian Academy of Sciences, Lazarettgasse 14, A-1090 Vienna, Austria;

    The Oulu Center for Cell-Matrix Research, Biocenter Oulu, Department of Medical Biochemistry and Molecular Biology, University ofOulu, FIN-90014, Oulu, Finland;

    Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, United Kingdom;

    Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, United Kingdom,The Botnar Research Center, NIHR, Oxford Biomedical Research Unit, Oxford OX3 7LD, United Kingdom;

    Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, United Kingdom,The Botnar Research Center, NIHR, Oxford Biomedical Research Unit, Oxford OX3 7LD, United Kingdom;

    Department of Chemistry and Biochemistry, University of Colorado, Boulder, Colorado 80309, United States;

    Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, United Kingdom,Astex Therapeutics, 436 Cambridge Science Park, Cambridge CB40QA, United Kingdom.;

    Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, United Kingdom,The Botnar Research Center, NIHR, Oxford Biomedical Research Unit, Oxford OX3 7LD, United Kingdom;

    The Howard Hughes Medical Institute at the Broad Institute of Harvard and MIT, 7 Cambridge Center, Cambridge, Massachusetts02142, United States,Department of Chemistry and Chemical Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, United States;

    Department of Chemistry and Biochemistry, University of Colorado, Boulder, Colorado 80309, United States;

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