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@article{Allott:2021:10.1039/d1re00117e,
author = {Allott, L and Amgheib, A and Barnes, C and Braga, M and Brickute, D and Wang, N and Fu, R and Ghaem-Maghami, S and Aboagye, EO},
doi = {10.1039/d1re00117e},
journal = {Reaction Chemistry and Engineering},
pages = {1070--1078},
title = {Radiolabelling an F-18 biologic via facile IEDDA "click" chemistry on the GE FASTLab (TM) platform},
url = {http://dx.doi.org/10.1039/d1re00117e},
volume = {6},
year = {2021}
}

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TY  - JOUR
AB  - The use of biologics in positron emission tomography (PET) imaging is an important area of radiopharmaceutical development and new automated methods are required to facilitate their production. We report an automated radiosynthesis method to produce a radiolabelled biologic via facile inverse electron demand Diels–Alder (IEDDA) “click” chemistry on a single GE FASTLab™ cassette. We exemplified the method by producing a fluorine-18 radiolabelled interleukin-2 (IL2) radioconjugate from a trans-cyclooctene (TCO) modified IL2 precursor. The radioconjugate was produced using a fully automated radiosynthesis on a single FASTLab™ cassette in a decay-corrected radiochemical yield (RCY, d.c.) of 19.8 ± 2.6% in 110 min (from start of synthesis); the molar activity was 132.3 ± 14.6 GBq μmol−1. The in vitro uptake of [18F]TTCO-IL2 correlated with the differential receptor expression (CD25, CD122, CD132) in PC3, NK-92 and activated human PBMCs. The automated method may be adapted for the radiosynthesis of any TCO-modified protein via IEDDA chemistry.
AU  - Allott,L
AU  - Amgheib,A
AU  - Barnes,C
AU  - Braga,M
AU  - Brickute,D
AU  - Wang,N
AU  - Fu,R
AU  - Ghaem-Maghami,S
AU  - Aboagye,EO
DO  - 10.1039/d1re00117e
EP  - 1078
PY  - 2021///
SN  - 2058-9883
SP  - 1070
TI  - Radiolabelling an F-18 biologic via facile IEDDA "click" chemistry on the GE FASTLab (TM) platform
T2  - Reaction Chemistry and Engineering
UR  - http://dx.doi.org/10.1039/d1re00117e
UR  - http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000642563400001&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=1ba7043ffcc86c417c072aa74d649202
UR  - https://pubs.rsc.org/en/content/articlelanding/2021/RE/D1RE00117E#!divAbstract
UR  - http://hdl.handle.net/10044/1/89785
VL  - 6
ER  -

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