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.
TidsskriftBioorganic & Medicinal Chemistry Letters
Udgave nummer18
Sider (fra-til)5811-3
Antal sider3
StatusUdgivet - 15 sep. 2012

ID: 45967576