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

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OHagan_2015_ChemComm_TwoStep_CC.pdf (1.742Mb)
Date
11/09/2015
Author
Thompson, Stephen
Ónega, Mayca
Ashworth, Sharon
Fleming , Ian N.
Passchier , Jan
O'Hagan, David
Funder
EPSRC
Grant ID
EP/I034734/1
Keywords
QD Chemistry
NDAS
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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 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.
Citation
Thompson , S , Ónega , M , Ashworth , S , Fleming , I N , Passchier , J & O'Hagan , D 2015 , ' A two-step fluorinase enzyme mediated 18 F labelling of an RGD peptide for positron emission tomography ' , Chemical Communications , vol. 51 , no. 70 , pp. 13542-13545 . https://doi.org/10.1039/C5CC05013H
Publication
Chemical Communications
Status
Peer reviewed
DOI
https://doi.org/10.1039/C5CC05013H
ISSN
1359-7345
Type
Journal article
Rights
Copyright 2015 the Authors. This article is licensed under a Creative Commons Attribution 3.0 Unported Licence (http://creativecommons.org/licenses/by/3.0/).
Description
The authors thank EPSRC and the Scottish Imaging Network (SINAPSE) for grants. DO’H thanks the Royal Society for a Wolfson Research Merit Award and ST is grateful to the John and Kathleen Watson Scholarship for financial support.
Collections
  • University of St Andrews Research
URL
http://www.rsc.org/suppdata/c5/cc/c5cc05013h/c5cc05013h1.pdf
URI
http://hdl.handle.net/10023/7790

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