Evaluation of micro-parallel liquid chromatography as a method for HTS-coupled actives verification.
|Abstract||The identification of biologically active compounds from high-throughput screening (HTS) can involve considerable postscreening analysis to verify the nature of the sample activity. In this study we evaluated the performance of micro-parallel liquid chromatography (microPLC) as a separation-based enzyme assay platform for follow-up of compound activities found in quantitative HTS of two different targets, a hydrolase and an oxidoreductase. In an ... [truncated at 450 characters in length]|
|Author||Simeonov, Anton; Yasgar, Adam; Klumpp, Carleen; et al|
|Subject||Chromatography, Gas Chromatography, High Pressure Liquid Chromatography, Liquid Dose-Response Relationship, Drug Drug Evaluation, Preclinical Enzyme Activation False Positive Reactions Fluorometry Glucosylceramidase Hydroxymethylglutaryl CoA Reductases Indicators and Reagents Spectrometry, Fluorescence Spectrophotometry, Ultraviolet methods instrumentation methods drug effects analysis metabolism analysis metabolism|
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|