4.7 Article

A fluopol-ABPP HTS assay to identify PAD inhibitors

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CHEMICAL COMMUNICATIONS
卷 46, 期 38, 页码 7175-7177

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c0cc02634d

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  1. University Of South Carolina
  2. TSRI, Scripps Florida
  3. National Institutes of Health [GM079357]
  4. NATIONAL CANCER INSTITUTE [R01CA132630] Funding Source: NIH RePORTER
  5. NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES [R01GM079357] Funding Source: NIH RePORTER

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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.

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