Document Report Card

ID: ALA2390894

Journal: J Med Chem

Title: Quantitative analysis of histone demethylase probes using fluorescence polarization.

Authors: Xu W, Podoll JD, Dong X, Tumber A, Oppermann U, Wang X.

Abstract: We previously reported methylstat as a selective inhibitor of jumonji C domain-containing histone demethylases (JHDMs). Herein, we describe the synthesis of a fluorescent analogue of methylstat and its application as a tracer in fluorescence polarization assays. Using this format, we have evaluated the binding affinities of several known JHDM probes, as well as the native cofactor and substrate of JHDM1A. This fluorophore allowed a highly robust and miniaturized competition assay sufficient for high-throughput screening.

CiteXplore: 23725560

DOI: 10.1021/jm3018628