A fluopol-ABPP HTS assay to identify PAD inhibitors

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Authors
Knuckley, Bryan
Jones, Justin E.
Bachovchin, Daniel A.
Slack, Jessica
Causey, Corey P.
Brown, Steven J.
Rosen, Hugh
Cravatt, Benjamin F.
Thompson, Paul R
UMass Chan Affiliations
Department of Biochemistry and Molecular Pharmacology
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

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Link to Full Text
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2943038/
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.
DOI
10.1039/c0cc02634d
Permanent Link to this Item
http://hdl.handle.net/20.500.14038/50049
Notes

At the time of publication, Paul Thompson was not yet affiliated with UMass Medical School.
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