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A fluopol-ABPP HTS assay to identify PAD inhibitors
Knuckley, Bryan ; Jones, Justin E. ; Bachovchin, Daniel A. ; Slack, Jessica ; Causey, Corey P. ; Brown, Steven J. ; Rosen, Hugh ; Cravatt, Benjamin F. ; Thompson, Paul R
Knuckley, Bryan
Jones, Justin E.
Bachovchin, Daniel A.
Slack, Jessica
Causey, Corey P.
Brown, Steven J.
Rosen, Hugh
Cravatt, Benjamin F.
Thompson, Paul R
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Student Authors
Faculty Advisor
Academic Program
UMass Chan Affiliations
Document Type
Journal Article
Publication Date
2010-10-14
Keywords
Arthritis, Rheumatoid
Cell Line, Tumor
Drug Evaluation, Preclinical
Enzyme Inhibitors
Fluorescence Polarization
Fluorescent Dyes
High-Throughput Screening Assays
Humans
Hydrolases
Inhibitory Concentration 50
Streptonigrin
Biochemistry
Enzymes and Coenzymes
Medicinal-Pharmaceutical Chemistry
Therapeutics
Cell Line, Tumor
Drug Evaluation, Preclinical
Enzyme Inhibitors
Fluorescence Polarization
Fluorescent Dyes
High-Throughput Screening Assays
Humans
Hydrolases
Inhibitory Concentration 50
Streptonigrin
Biochemistry
Enzymes and Coenzymes
Medicinal-Pharmaceutical Chemistry
Therapeutics
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Embargo Expiration Date
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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.
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.
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DOI
10.1039/c0cc02634d
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Notes
At the time of publication, Paul Thompson was not yet affiliated with UMass Medical School.