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

Stephen Thompson, Mayca Ónega, Sharon Ashworth, Ian N. Fleming , Jan Passchier , David O'Hagan

Research output: Contribution to journalArticlepeer-review

21 Citations (Scopus)
1 Downloads (Pure)

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 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.

Original languageEnglish
Pages (from-to)13542-13545
JournalChemical Communications
Volume51
Issue number70
Early online date17 Jul 2015
DOIs
Publication statusPublished - 11 Sept 2015

Fingerprint

Dive into the research topics of 'A two-step fluorinase enzyme mediated 18F labelling of an RGD peptide for positron emission tomography'. Together they form a unique fingerprint.

Cite this