1H NMR-based assay for lysine demethylase LSD1 and its application to inhibitor screening

Lysine-specific demethylase 1 (LSD1) with oxidation activity that relies on flavin adenine dinucleotide (FAD) to subsequently produce formaldehyde have been associated with various types of cancers. Here, we report an NMR-based assay for detecting the LSD1 enzyme activity. Our approach can be performed in a reaction buffer without any extraction step, achieve a time-dependent absolute quantification, and be useful for the enzyme inhibitor screening. This precise assay allows us to develop new inhibitors of the LSD1 as anticancer agents.