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18F-Labeling of Radiotracers Functionalized with a Silicon Fluoride Acceptor SiFA for Positron Emission Tomography
Published on: January 11, 2020
A two-step fluorinase enzyme mediated (18)F labelling of an RGD peptide for positron emission tomography
S Thompson1, M Onega, S Ashworth
1School of Chemistry, University of St Andrews, North Haugh, St Andrews, KY16 9ST, UK. do1@st-andrews.ac.uk.
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 [(18)F]-5'-fluoro-5'-deoxy-2-ethynyladenosine, [(18)F]FDEA, followed by a 'click' reaction to an azide tethered cRGD peptide. This protocol offers efficient radiolabelling of a biologically relevant peptide construct in water at pH 7.8, 37 °C in 2 hours, which was metabolically stable in rats and retained high affinity for αVβ3 integrin.
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