Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C)
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The human histone demethylases of the KDM4 (JMJD2) family have been associated to diseases such as prostate and breast cancer, as well as X-linked mental retardation. Therefore, these enzymes are considered oncogenes and their selective inhibition might be a possible therapeutic approach to treat cancer. Here we describe a heterocyclic ring system library screened against the histone demethylase KDM4C (JMJD2C) in the search for novel inhibitory scaffolds. A 4-hydroxypyrazole scaffold was identified as an inhibitor of KDM4C; this scaffold could be employed in the further development of novel therapeutics, as well as for the elucidation of the biological roles of KDM4C on epigenetic regulation.
|Journal||Bioorganic & Medicinal Chemistry Letters|
|Number of pages||3|
|Publication status||Published - 15 Sep 2012|
- Dose-Response Relationship, Drug, Drug Design, Enzyme Inhibitors, Humans, Jumonji Domain-Containing Histone Demethylases, Molecular Structure, Pyrazoles, Small Molecule Libraries, Structure-Activity Relationship