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Quantitative analysis of histone demethylase probes using fluorescence polarization.

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

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

doi

10.1021/jm3018628

subject

Has Abstract

pub_date

2013-06-27 00:00:00

pages

5198-202

issue

12

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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