A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography
MetadataShow full item record
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/).
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.
Items in the St Andrews Research Repository are protected by copyright, with all rights reserved, unless otherwise indicated.