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@ARTICLE{Grner:1026693,
author = {Gröner, Benedikt and Hoffmann, Chris and Endepols, Heike
and Urusova, Elizaveta and Brugger, Melanie and Neumaier,
Felix and Timmer, Marco and Neumaier, Bernd and
Zlatopolskiy, Boris D.},
title = {{R}adiosynthesis and {P}reclinical {E}valuation of
m-[18{F}]{FET} and [18{F}]{FET}-{OM}e as {N}ovel
[18{F}]{FET} {A}nalogs for {B}rain {T}umor {I}maging},
journal = {Molecular pharmaceutics},
volume = {21},
issn = {1543-8384},
address = {Washington, DC},
publisher = {American Chemical Society},
reportid = {FZJ-2024-03507},
pages = {2795-2812},
year = {2024},
note = {This work was supported, in part, by
DeutscheForschungsgemeinschaft (DFG) grants ZL 65/1-1, ZL
65/3-1,and ZL 65/4-1.},
abstract = {O-([18F]Fluoroethyl)-L-tyrosine ([18F]FET) is
activelytransported into the brain and cancer cells by LAT1
andpossibly other amino acid transporters, which enables
brain tumorimaging by positron emission tomography (PET).
However, tumordelivery of this probe in the presence of
competing amino acidsmay be limited by a relatively low
affinity for LAT1. The aim of thepresent work was to
evaluate the meta-substituted [18F]FET analogm-[18F]FET and
the methyl ester [18F]FET-OMe, which weredesigned to improve
tumor delivery by altering the
physicochemical,pharmacokinetic, and/or transport
properties. Both tracerscould be prepared with good
radiochemical yields of $41−56\%within$ 66−90 min.
Preclinical evaluation with [18F]FET as areference tracer
demonstrated reduced in vitro uptake of [18F]FETOMeby U87
glioblastoma cells and no advantage for in vivo tumor
imaging. In contrast, m-[18F]FET showed significantly
improvedin vitro uptake and accelerated in vivo tumor
accumulation in an orthotopic glioblastoma model. As such,
our work identifies m-[18F]FET as a promising alternative to
[18F]FET for brain tumor imaging that deserves further
evaluation with regard to its transportproperties and in
vivo biodistribution.},
cin = {INM-5},
ddc = {610},
cid = {I:(DE-Juel1)INM-5-20090406},
pnm = {5253 - Neuroimaging (POF4-525)},
pid = {G:(DE-HGF)POF4-5253},
typ = {PUB:(DE-HGF)16},
pubmed = {38747353},
UT = {WOS:001225916700001},
doi = {10.1021/acs.molpharmaceut.3c01215},
url = {https://juser.fz-juelich.de/record/1026693},
}