A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography
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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.
Thompson , 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 . DOI: 10.1039/C5CC05013H
Copyright 2015 the Authors. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence (http://creativecommons.org/licenses/by/3.0/).
The 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.
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