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A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.

Publication TypeJournal Article
AuthorsLuo, X., Liu Y., Kubicek S., Myllyharju J., Tumber A., Ng S., Che KH, Podoll J., Heightman TD, Oppermann U., Schreiber SL, and Wang X.
AbstractHistone 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.
Year of Publication2011
JournalJournal of the American Chemical Society
Volume133
Issue24
Pages9451-6
Date Published (YYYY/MM/DD)2011/06/22
ISSN Number0002-7863
DOI10.1021/ja201597b
PubMedhttp://www.ncbi.nlm.nih.gov/pubmed/21585201?dopt=Abstract