Ontology highlight
ABSTRACT:
SUBMITTER: Luo X
PROVIDER: S-EPMC3133600 | biostudies-literature | 2011 Jun
REPOSITORIES: biostudies-literature
Journal of the American Chemical Society 20110531 24
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, ...[more]