A miniaturized screen for inhibitors of Jumonji histone demethylases.
|Abstract||2-Oxoglutarate- and Fe(ii)-dependent oxygenases are a major class of N(epsilon)-methyl lysine demethylases that are involved in epigenetic regulation. Assays suitable for implementation in a high-throughput manner have been lacking for these enzymes. Here, we describe the design and implementation of a robust and miniaturized high-throughput kinetic assay for inhibitors of JMJD2E using a formaldehyde dehydrogenase-coupled reaction with real-time ... [truncated at 450 characters in length]|
|Author||Sakurai, Masaaki; Rose, Nathan R; Schultz, Lena; et al|
|Subject||Aldehyde Oxidoreductases Drug Discovery Enzyme Inhibitors Humans Jumonji Domain-Containing Histone Demethylases Kinetics Miniaturization Spectrometry, Fluorescence Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization metabolism methods pharmacology antagonists and inhibitors metabolism methods methods|