Issue 38, 2010

A fluopol-ABPP HTS assay to identify PADinhibitors

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

Supplementary files

Article information

Article type
Communication
Submitted
17 Jul 2010
Accepted
30 Jul 2010
First published
25 Aug 2010

Chem. Commun., 2010,46, 7175-7177

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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