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@ARTICLE{Willuweit:1005300,
author = {Willuweit, Antje and Humpert, Swen and Schöneck, Michael
and Endepols, Heike and Burda, Nicole and Gremer, Lothar and
Gering, Ian and Kutzsche, Janine and Shah, N. Jon and
Langen, Karl-Josef and Neumaier, Bernd and Willbold, Dieter
and Drzezga, Alexander},
title = {{E}valuation of the 18{F}-{L}abeled {A}nalog of the
{T}herapeutic {A}ll-d-enantiomeric {P}eptide {RD}2 for
{A}myloid β {I}maging},
journal = {European journal of pharmaceutical sciences},
volume = {184},
issn = {0928-0987},
address = {New York, NY [u.a.]},
publisher = {Elsevier},
reportid = {FZJ-2023-01412},
pages = {106421},
year = {2023},
abstract = {Positron emission tomography (PET) imaging with
radiotracers that bind to fibrillary amyloid β (Aβ)
deposits is an important tool for the diagnosis of
Alzheimer's disease (AD) and for the recruitment of patients
into clinical trials. However, it has been suggested that
rather than the fibrillary Aβ deposits, it is smaller,
soluble Aβ aggregates that exert a neurotoxic effect and
trigger AD pathogenesis. The aim of the current study is to
develop a PET probe that is capable of detecting small
aggregates and soluble Aβ oligomers for improved diagnosis
and therapy monitoring. An 18F-labeled radioligand was
prepared based on the Aβ-binding d-enantiomeric peptide
RD2, which is currently being evaluated in clinical trials
as a therapeutic agent to dissolve Aβ oligomers.
18F-labeling was carried out using palladium-catalyzed
S-arylation of RD2 with 2-[18F]fluoro-5-iodopyridine
([18F]FIPy). Specific binding of [18F]RD2-cFPy to brain
material from transgenic AD (APP/PS1) mice and AD patients
was demonstrated with in vitro autoradiography. In vivo
uptake and biodistribution of [18F]RD2-cFPy were evaluated
using PET analyses in wild-type and transgenic APP/PS1 mice.
Although brain penetration and brain wash-out kinetics of
the radioligand were low, this study provides proof of
principle for a PET probe based on a d-enantiomeric peptide
binding to soluble Aβ species.},
cin = {INM-4 / INM-5 / IBI-7 / INM-2 / INM-11 / JARA-BRAIN},
ddc = {610},
cid = {I:(DE-Juel1)INM-4-20090406 / I:(DE-Juel1)INM-5-20090406 /
I:(DE-Juel1)IBI-7-20200312 / I:(DE-Juel1)INM-2-20090406 /
I:(DE-Juel1)INM-11-20170113 / $I:(DE-82)080010_20140620$},
pnm = {5253 - Neuroimaging (POF4-525) / 5244 - Information
Processing in Neuronal Networks (POF4-524) / 5252 - Brain
Dysfunction and Plasticity (POF4-525)},
pid = {G:(DE-HGF)POF4-5253 / G:(DE-HGF)POF4-5244 /
G:(DE-HGF)POF4-5252},
typ = {PUB:(DE-HGF)16},
pubmed = {36889654},
UT = {WOS:000956437600001},
doi = {10.1016/j.ejps.2023.106421},
url = {https://juser.fz-juelich.de/record/1005300},
}