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Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. Epub 2010 Aug 25.

A fluopol-ABPP HTS assay to identify PAD inhibitors.

Author information

1
Department of Chemistry, The Scripps Research Institute, Scripps Florida, 120 Scripps Way, Jupiter, Florida, USA33458.

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.

PMID:
20740228
PMCID:
PMC2943038
DOI:
10.1039/c0cc02634d
[Indexed for MEDLINE]
Free PMC Article

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