Histone demethylase (null)

Histone demethylases are enzymes responsible for removing methyl groups from lysine or arginine residues on histone proteins, which directly alter chromatin structure and regulate gene expression. They play crucial roles in epigenetic modification, orchestrating transcriptional activation or repression, cell fate, differentiation, and development. Two main classes exist: FAD-dependent amine oxidases (e.g., KDM1A/LSD1) and 2-oxoglutarate/Fe(II)-dependent Jumonji C domain (JmjC) oxygenases (e.g., KDM2A, KDM6A). Dysregulation or mutation of histone demethylases is implicated in cancer, neurodevelopmental syndromes, and other diseases, making them significant therapeutic targets for epigenetic drugs. Note: "Histone demethylase" is not a specific single molecular target but a family name covering many enzymes (e.g., LSD1/KDM1A, KDM6A/UTX, etc.). For drug discovery or structured data, mapping to a specific demethylase gene/protein is critical.

Other names

histone lysine demethylaseKDMJMJDlysine-specific demethylasedemethylase

Inhibition of demethylase activity—prevents demethylation of histone lysine residues, alters gene expression. Some covalently modify cofactor (e.g., FAD-binding inhibition for KDM1A). Dimethylation state–specific inhibition for some drugs.