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Fluorinated Phosphoadenosine 5′-Phosphosulfate Analogues for Continuous Sulfotransferase Activity Monitoring and Inhibitor Screening by <sup>19</sup>F NMR Spectroscopy

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dc.abstract.enSulfotransferases (STs) are ubiquitous enzymes that participate in a vast number of biological processes involving sulfuryl group (SO3) transfer. 3′-phosphoadenosine 5′-phosphosulfate (PAPS) is the universal ST cofactor, serving as the “active sulfate” source in cells. Herein, we report the synthesis of three fluorinated PAPS analogues that bear fluorine or trifluoromethyl substituents at the C2 or C8 positions of adenine and their evaluation as substitute cofactors that enable ST activity to be quantified and real-time-monitored by fluorine-19 nuclear magnetic resonance (19F NMR) spectroscopy. Using plant AtSOT18 and human SULT1A3 as two model enzymes, we reveal that the fluorinated PAPS analogues show complementary properties with regard to recognition by enzymes and the working 19F NMR pH range and are attractive versatile tools for studying STs. Finally, we developed an 19F NMR assay for screening potential inhibitors against SULT1A3, thereby highlighting the possible use of fluorinated PAPS analogues for the discovery of drugs for ST-related diseases.
dc.affiliationUniwersytet Warszawski
dc.contributor.authorKowalska, Joanna
dc.contributor.authorJemielity, Jacek
dc.contributor.authorBednarczyk, Marcelina
dc.contributor.authorBaranowski, Marek R.
dc.contributor.authorSpiewla, Tomasz
dc.contributor.authorChrominski, Mikolaj
dc.contributor.authorMlynarska-Cieslak, Agnieszka
dc.date.accessioned2024-01-25T01:13:59Z
dc.date.available2024-01-25T01:13:59Z
dc.date.issued2022
dc.description.financePublikacja bezkosztowa
dc.description.number3
dc.description.volume17
dc.identifier.doi10.1021/ACSCHEMBIO.1C00978
dc.identifier.issn1554-8929
dc.identifier.urihttps://repozytorium.uw.edu.pl//handle/item/107307
dc.identifier.weblinkhttps://pubs.acs.org/doi/pdf/10.1021/acschembio.1c00978
dc.languageeng
dc.pbn.affiliationchemical sciences
dc.relation.ispartofACS Chemical Biology
dc.relation.pages661-669
dc.rightsClosedAccess
dc.sciencecloudnosend
dc.titleFluorinated Phosphoadenosine 5′-Phosphosulfate Analogues for Continuous Sulfotransferase Activity Monitoring and Inhibitor Screening by <sup>19</sup>F NMR Spectroscopy
dc.typeJournalArticle
dspace.entity.typePublication