A fluopol-ABPP HTS assay to identify PAD inhibitors
dc.contributor.author | Knuckley, Bryan | |
dc.contributor.author | Jones, Justin E. | |
dc.contributor.author | Bachovchin, Daniel A. | |
dc.contributor.author | Slack, Jessica | |
dc.contributor.author | Causey, Corey P. | |
dc.contributor.author | Brown, Steven J. | |
dc.contributor.author | Rosen, Hugh | |
dc.contributor.author | Cravatt, Benjamin F. | |
dc.contributor.author | Thompson, Paul R | |
dc.date | 2022-08-11T08:11:00.000 | |
dc.date.accessioned | 2022-08-23T17:28:18Z | |
dc.date.available | 2022-08-23T17:28:18Z | |
dc.date.issued | 2010-10-14 | |
dc.date.submitted | 2015-05-27 | |
dc.identifier.citation | Chem Commun (Camb). 2010 Oct 14;46(38):7175-7. doi: 10.1039/c0cc02634d. <a href="http://dx.doi.org/10.1039/c0cc02634d">Link to article on publisher's site</a>. Epub 2010 Aug 25. | |
dc.identifier.issn | 1359-7345 (Linking) | |
dc.identifier.doi | 10.1039/c0cc02634d | |
dc.identifier.uri | http://hdl.handle.net/20.500.14038/50049 | |
dc.description | <p>At the time of publication, Paul Thompson was not yet affiliated with UMass Medical School.</p> | |
dc.description.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. | |
dc.language.iso | en_US | |
dc.relation | <a href="http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?db=pubmed&cmd=Retrieve&list_uids=20740228&dopt=Abstract">Link to Article in PubMed</a> | |
dc.relation.url | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2943038/ | |
dc.subject | Arthritis, Rheumatoid | |
dc.subject | Cell Line, Tumor | |
dc.subject | Drug Evaluation, Preclinical | |
dc.subject | Enzyme Inhibitors | |
dc.subject | Fluorescence Polarization | |
dc.subject | Fluorescent Dyes | |
dc.subject | High-Throughput Screening Assays | |
dc.subject | Humans | |
dc.subject | Hydrolases | |
dc.subject | Inhibitory Concentration 50 | |
dc.subject | Streptonigrin | |
dc.subject | Biochemistry | |
dc.subject | Enzymes and Coenzymes | |
dc.subject | Medicinal-Pharmaceutical Chemistry | |
dc.subject | Therapeutics | |
dc.title | A fluopol-ABPP HTS assay to identify PAD inhibitors | |
dc.type | Journal Article | |
dc.source.journaltitle | Chemical communications (Cambridge, England) | |
dc.source.volume | 46 | |
dc.source.issue | 38 | |
dc.identifier.legacyfulltext | https://escholarship.umassmed.edu/cgi/viewcontent.cgi?article=1056&context=thompson&unstamped=1 | |
dc.identifier.legacycoverpage | https://escholarship.umassmed.edu/thompson/57 | |
dc.identifier.contextkey | 7144791 | |
refterms.dateFOA | 2022-08-23T17:28:18Z | |
html.description.abstract | <p>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.</p> | |
dc.identifier.submissionpath | thompson/57 | |
dc.contributor.department | Department of Biochemistry and Molecular Pharmacology | |
dc.source.pages | 7175-7 |