This week in techniques



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Assays & screens

Quantitative analysis of jumonji C domain-containing histone demethylase (JHDM)-targeting compounds

An assay for quantitative analysis of JHDM inhibitor activity could aid the development of lead compounds that target the class of enzymes. A fluorescent analog of a previously identified selective inhibitor of JHDMs was synthesized and used as a tracer molecule in a fluorescence polarization binding assay. The assay enabled quantitative assessments of the binding affinity and inhibitory activity of multiple JHDM chemical probes. Next steps include developing a panel of fluorescence polarization assays for additional JHDMs and using them to determine the specificity of additional JHDM probes.

SciBX 6(25); doi:10.1038/scibx.2013.636
Published online June 27, 2013

Unpatented; licensing status not applicable

Xu, W. et al. J. Med. Chem.;
published online May 30, 2013;
Contact: Xiang Wang, University of Colorado at Boulder, Boulder, Colo.