An Overview on Screening Methods for Lysine Specific Demethylase 1 (LSD1) Inhibitors

Background: In the past few years, great of attention has been paid to the identification and characterization of selective and potent inhibitors of the first identified histone demethylase LSD1, which may erase mono- and di-methylated histone 3 lysine 4 and 9. As the aberrant overexpression of LSD1 is involved in various pathological processes, especially cancer, obtaining selective and potent LSD1 inhibitors has emerged as a crucial issue in medicinal chemistry research. Keywords: LSD1, inhibitor, screening model, enzyme coupled assay, LC-MS, FRET.