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dc.contributor.authorAskin, Samuel
dc.contributor.authorBond, Thomas EH
dc.contributor.authorSorenson, Alanna E
dc.contributor.authorMoreau, Morgane JJ
dc.contributor.authorAntony, Helma
dc.contributor.authorDavis, Rohan A
dc.contributor.authorSchaeffer, Patrick M
dc.date.accessioned2019-05-29T13:04:36Z
dc.date.available2019-05-29T13:04:36Z
dc.date.issued2018
dc.identifier.issn1359-7345
dc.identifier.doi10.1039/c8cc00090e
dc.identifier.urihttp://hdl.handle.net/10072/379894
dc.description.abstractHigh-throughput differential scanning fluorimetry of GFP-tagged proteins (HT-DSF-GTP) was applied for the identification of novel enzyme inhibitors acting by a mechanism termed: selective protein unfolding (SPU). Four different protein targets were interrogated with the same library to identify target-selective hits. Several hits selectively destabilized bacterial biotin protein ligase. Structure–activity relationship data confirmed a structure-dependent mechanism of protein unfolding. Simvastatin and altenusin were confirmed to irreversibly inactivate biotin protein ligase. The principle of SPU combined with HT-DSF-GTP affords an invaluable and innovative workflow for the identification of new inhibitors with potential applications as antimicrobials and other biocides.
dc.description.peerreviewedYes
dc.languageEnglish
dc.publisherRoyal Society of Chemistry
dc.publisher.placeUnited Kingdom
dc.relation.ispartofpagefrom1738
dc.relation.ispartofpageto1741
dc.relation.ispartofissue14
dc.relation.ispartofjournalChemical Communications
dc.relation.ispartofvolume54
dc.subject.fieldofresearchChemical Sciences not elsewhere classified
dc.subject.fieldofresearchChemical Sciences
dc.subject.fieldofresearchcode039999
dc.subject.fieldofresearchcode03
dc.titleSelective protein unfolding: a universal mechanism of action for the development of irreversible inhibitors
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorDavis, Rohan A.


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