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., Onega, M., Ashworth, S., Fleming, I. N., Passchier, J., & O'Hagan, D. (2015). A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography. Chemical Communications, 51(70), 13542-13545. https://doi.org/10.1039/C5CC05013H