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

S. Thompson, M. Onega, S. Ashworth, I. N. Fleming, J. Passchier, D. O'Hagan (Corresponding Author)

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Abstract

A 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.
Original languageEnglish
Pages (from-to)13542-13545
Number of pages4
JournalChemical Communications
Volume51
Issue number70
Early online date17 Jul 2015
DOIs
Publication statusPublished - 2015

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