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Issue 70, 2015
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A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography

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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

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Publication details

The article was received on 17 Jun 2015, accepted on 16 Jul 2015 and first published on 17 Jul 2015


Article type: Communication
DOI: 10.1039/C5CC05013H
Citation: Chem. Commun., 2015,51, 13542-13545
  • Open access: Creative Commons BY license
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    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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