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A fluopol-ABPP HTS assay to identify PAD inhibitors.

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.

SUBMITTER: Knuckley B 

PROVIDER: S-EPMC2943038 | biostudies-literature | 2010 Oct

REPOSITORIES: biostudies-literature

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A fluopol-ABPP HTS assay to identify PAD inhibitors.

Knuckley Bryan B   Jones Justin E JE   Bachovchin Daniel A DA   Slack Jessica J   Causey Corey P CP   Brown Steven J SJ   Rosen Hugh H   Cravatt Benjamin F BF   Thompson Paul R PR  

Chemical communications (Cambridge, England) 20100825 38

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. ...[more]

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