A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography. Issue 70 (29th July 2015)

• Record Type: Journal Article
• Authors: Thompson, S.; Onega, M.; Ashworth, S.; Fleming, I. N.; Passchier, J.; O'Hagan, D.
• Is Part Of: Chemical communications. Volume 51:Issue 70(2015)
• Page Start: 13542
• Page End: 13545
• Publication Date: 2015-07-29
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/c5cc05013h
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Fluorine-18 radiolabelling of a peptide is conducted in water (pH 7.8 and 37 °C) using the fluorinase enzyme and a 'click' reaction. 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 αV β3 integrin.