Title
A fluopol-ABPP HTS assay to identify PAD inhibitors
UMMS Affiliation
Department of Biochemistry and Molecular Pharmacology
Publication Date
2010-10-14
Document Type
Article
Subjects
Arthritis, Rheumatoid; Cell Line, Tumor; Drug Evaluation, Preclinical; Enzyme Inhibitors; Fluorescence Polarization; Fluorescent Dyes; High-Throughput Screening Assays; Humans; Hydrolases; Inhibitory Concentration 50; Streptonigrin
Disciplines
Biochemistry | Enzymes and Coenzymes | Medicinal-Pharmaceutical Chemistry | Therapeutics
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.
DOI of Published Version
10.1039/c0cc02634d
Source
Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. Link to article on publisher's site. Epub 2010 Aug 25.
Journal/Book/Conference Title
Chemical communications (Cambridge, England)
Related Resources
Repository Citation
Knuckley, Bryan; Jones, Justin E.; Bachovchin, Daniel A.; Slack, Jessica; Causey, Corey P.; Brown, Steven J.; Rosen, Hugh; Cravatt, Benjamin F.; and Thompson, Paul R., "A fluopol-ABPP HTS assay to identify PAD inhibitors" (2010). Thompson Lab Publications. 57.
https://escholarship.umassmed.edu/thompson/57
Comments
At the time of publication, Paul Thompson was not yet affiliated with UMass Medical School.