We are upgrading the repository! A content freeze is in effect until December 6, 2024. New submissions or changes to existing items will not be allowed during this period. All content already published will remain publicly available for searching and downloading. Updates will be posted in the Website Upgrade 2024 FAQ in the sidebar Help menu. Reach out to escholarship@umassmed.edu with any questions.

Show simple item record

dc.contributor.authorKnuckley, Bryan
dc.contributor.authorJones, Justin E.
dc.contributor.authorBachovchin, Daniel A.
dc.contributor.authorSlack, Jessica
dc.contributor.authorCausey, Corey P.
dc.contributor.authorBrown, Steven J.
dc.contributor.authorRosen, Hugh
dc.contributor.authorCravatt, Benjamin F.
dc.contributor.authorThompson, Paul R
dc.date2022-08-11T08:11:00.000
dc.date.accessioned2022-08-23T17:28:18Z
dc.date.available2022-08-23T17:28:18Z
dc.date.issued2010-10-14
dc.date.submitted2015-05-27
dc.identifier.citationChem 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.issn1359-7345 (Linking)
dc.identifier.doi10.1039/c0cc02634d
dc.identifier.urihttp://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.abstractProtein 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.isoen_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.urlhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC2943038/
dc.subjectArthritis, Rheumatoid
dc.subjectCell Line, Tumor
dc.subjectDrug Evaluation, Preclinical
dc.subjectEnzyme Inhibitors
dc.subjectFluorescence Polarization
dc.subjectFluorescent Dyes
dc.subjectHigh-Throughput Screening Assays
dc.subjectHumans
dc.subjectHydrolases
dc.subjectInhibitory Concentration 50
dc.subjectStreptonigrin
dc.subjectBiochemistry
dc.subjectEnzymes and Coenzymes
dc.subjectMedicinal-Pharmaceutical Chemistry
dc.subjectTherapeutics
dc.titleA fluopol-ABPP HTS assay to identify PAD inhibitors
dc.typeJournal Article
dc.source.journaltitleChemical communications (Cambridge, England)
dc.source.volume46
dc.source.issue38
dc.identifier.legacyfulltexthttps://escholarship.umassmed.edu/cgi/viewcontent.cgi?article=1056&amp;context=thompson&amp;unstamped=1
dc.identifier.legacycoverpagehttps://escholarship.umassmed.edu/thompson/57
dc.identifier.contextkey7144791
refterms.dateFOA2022-08-23T17:28:18Z
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.submissionpaththompson/57
dc.contributor.departmentDepartment of Biochemistry and Molecular Pharmacology
dc.source.pages7175-7


Files in this item

Thumbnail
Name:
c0cc02634d.pdf
Size:
1.171Mb
Format:
PDF

This item appears in the following Collection(s)

Show simple item record