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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.accessioned2021-05-25T05:32:42Z
dc.date.available2021-05-25T05:32:42Z
dc.date.issued2018
dc.identifier.issn1359-7345en_US
dc.identifier.doi10.1039/c8cc00090een_US
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.en_US
dc.description.peerreviewedYesen_US
dc.languageEnglishen_US
dc.language.isoeng
dc.publisherRoyal Society of Chemistryen_US
dc.publisher.placeUnited Kingdom
dc.relation.ispartofpagefrom1738en_US
dc.relation.ispartofpageto1741en_US
dc.relation.ispartofissue14en_US
dc.relation.ispartofjournalChemical Communicationsen_US
dc.relation.ispartofvolume54en_US
dc.subject.fieldofresearchChemical Sciences not elsewhere classifieden_US
dc.subject.fieldofresearchChemical Sciencesen_US
dc.subject.fieldofresearchcode039999en_US
dc.subject.fieldofresearchcode03en_US
dc.titleSelective protein unfolding: a universal mechanism of action for the development of irreversible inhibitorsen_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Articlesen_US
dc.type.codeC - Journal Articlesen_US
dcterms.licensehttps://creativecommons.org/licenses/by-nc/3.0/en_US
dc.description.versionVersion of Record (VoR)en_US
gro.rights.copyright© The Author(s) 2018. This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial 3.0 Unported (CC BY-NC 3.0) License, which permits unrestricted, non-commercial use, distribution and reproduction in any medium, providing that the work is properly cited.en_US
gro.hasfulltextFull Text
gro.griffith.authorDavis, Rohan A.


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