A fluopol-ABPP HTS assay to identify PAD inhibitors.
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ABSTRACT:
SUBMITTER: Knuckley B
PROVIDER: S-EPMC2943038 | biostudies-literature | 2010 Oct
REPOSITORIES: biostudies-literature
Publications
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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