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Issue 38, 2010
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A fluopol-ABPP HTS assay to identify PAD inhibitors

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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.

Graphical abstract: A fluopol-ABPP HTS assay to identify PAD inhibitors

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Publication details

The article was received on 17 Jul 2010, accepted on 30 Jul 2010 and first published on 25 Aug 2010


Article type: Communication
DOI: 10.1039/C0CC02634D
Citation: Chem. Commun., 2010,46, 7175-7177
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    A fluopol-ABPP HTS assay to identify PAD inhibitors

    B. Knuckley, J. E. Jones, D. A. Bachovchin, J. Slack, C. P. Causey, S. J. Brown, H. Rosen, B. F. Cravatt and P. R. Thompson, Chem. Commun., 2010, 46, 7175
    DOI: 10.1039/C0CC02634D

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