Demethylases are enzymes that remove methyl groups from histones and other proteins, thereby regulating gene expression and chromatin structure. Two well-known demethylases include LSD (Lysine-Specific Demethylase) and FTO (Fat Mass and Obesity-Associated Protein), both of which play critical roles in health and disease. LSD1, for instance, removes methyl groups from histone H3, influencing chromatin structure and gene repression—a function that has made it a target in cancer therapy, especially in leukemia and other malignancies. FTO, on the other hand, is a key RNA demethylase involved in metabolic regulation. Mutations in FTO have been linked to obesity and metabolic disorders, making it a promising target for metabolic disease therapies. Together, LSD and FTO exemplify the potential of demethylase inhibitors as epigenetic therapies aimed at modulating disease pathways by altering gene expression patterns.

Demethylase Assays

Our demethylase assays use AlphaLISA and luminescence technology to provide high-sensitivity, non-radioactive readouts of demethylase activity.