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A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography

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dc.contributor.authorThompson, Stephen
dc.contributor.authorÓnega, Mayca
dc.contributor.authorAshworth, Sharon
dc.contributor.authorFleming , Ian N.
dc.contributor.authorPasschier , Jan
dc.contributor.authorO'Hagan, David
dc.date.accessioned2015-11-16T14:40:03Z
dc.date.available2015-11-16T14:40:03Z
dc.date.issued2015-09-11
dc.identifier203899096
dc.identifierfc515502-5526-4906-a17e-77b4f287ae97
dc.identifier84939865049
dc.identifier000359951200026
dc.identifier.citationThompson , S , Ónega , M , Ashworth , S , Fleming , I N , Passchier , J & O'Hagan , D 2015 , ' A two-step fluorinase enzyme mediated 18 F labelling of an RGD peptide for positron emission tomography ' , Chemical Communications , vol. 51 , no. 70 , pp. 13542-13545 . https://doi.org/10.1039/C5CC05013Hen
dc.identifier.issn1359-7345
dc.identifier.otherORCID: /0000-0002-0510-5552/work/68281279
dc.identifier.urihttps://hdl.handle.net/10023/7790
dc.descriptionThe authors thank EPSRC and the Scottish Imaging Network (SINAPSE) for grants. DO’H thanks the Royal Society for a Wolfson Research Merit Award and ST is grateful to the John and Kathleen Watson Scholarship for financial support.en
dc.description.abstractA two-step radiolabelling protocol of a cancer relevant cRGD peptide is described where the fluorinase enzyme is used to catalyse a transhalogenation reaction to generate [18F]-5'-fluoro-5'-deoxy-2-ethynyladenosine, [18F]FDEA, followed by a ‘click’ reaction to an azide tethered cRGD peptide. This protocol offers an efficient radiolabelling of a biologically relevant peptide construct in water at pH 7.8, 37oC in 2 hours, that was metabolically stable in rats and retained high affinity for the αVβ3 integrin.
dc.format.extent1827594
dc.language.isoeng
dc.relation.ispartofChemical Communicationsen
dc.subjectQD Chemistryen
dc.subjectNDASen
dc.subjectSDG 3 - Good Health and Well-beingen
dc.subject.lccQDen
dc.titleA two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomographyen
dc.typeJournal articleen
dc.contributor.sponsorEPSRCen
dc.contributor.institutionUniversity of St Andrews. School of Chemistryen
dc.contributor.institutionUniversity of St Andrews. EaSTCHEMen
dc.contributor.institutionUniversity of St Andrews. Biomedical Sciences Research Complexen
dc.identifier.doi10.1039/C5CC05013H
dc.description.statusPeer revieweden
dc.identifier.urlhttp://www.rsc.org/suppdata/c5/cc/c5cc05013h/c5cc05013h1.pdfen
dc.identifier.grantnumberEP/I034734/1en


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