A fluopol-ABPP HTS assay to identify PAD inhibitors
Chemical Communications2010Vol. 46(38), pp. 7175–7175
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Bryan Knuckley, Justin E. Jones, Daniel A. Bachovchin, Jessica L. Slack, Corey P. Causey, Steven J Brown, Hugh Rosen, Benjamin F. Cravatt, Paul R. Thompson
Abstract
Protein Arginine Deiminase (PAD) activity is dysregulated in numerous diseases, e.g., Rheumatoid Arthritis. Herein we describe the development of a fluorescence polarization-Activity Based Protein Profiling (fluopol-ABPP) based high throughput screening assay that can be used to identify PAD-selective inhibitors. Using this assay, streptonigrin was identified as a potent, selective, and irreversible PAD4 inactivator.
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