Issue 70, 2015

A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography

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 [18F]-5′-fluoro-5′-deoxy-2-ethynyladenosine, [18F]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.

Graphical abstract: A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography

Supplementary files

Article information

Article type
Communication
Submitted
17 Jun 2015
Accepted
16 Jul 2015
First published
17 Jul 2015
This article is Open Access
Creative Commons BY license

Chem. Commun., 2015,51, 13542-13545

A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography

S. Thompson, M. Onega, S. Ashworth, I. N. Fleming, J. Passchier and D. O'Hagan, Chem. Commun., 2015, 51, 13542 DOI: 10.1039/C5CC05013H

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