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Lysine-specific demethylase 4 (KDM4), also known as the JMJD2 family, is a subfamily of histone lysine demethylases that play a crucial role in epigenetic regulation by removing methyl groups from specific lysine residues on histone proteins. This activity modulates chromatin structure and gene expression, impacting diverse biological processes. Aberrant expression or amplification of KDM4 genes is linked to various cancers, where it may promote oncogene expression or suppress tumor suppressors through epigenetic mechanisms. Several small-molecule inhibitors have been developed targeting the catalytic site or substrate recognition regions. These inhibitors show potential for therapeutic intervention by blocking aberrant gene activation/silencing pathways driven by dysregulated demethylation activity.
Inhibition of histone demethylation
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