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@ARTICLE{Shojaei:269527,
author = {Shojaei, Monireh and Zhou, Qihui and Palumbo, Giovanna and
Schaefer, Rebecca and Kaskinoro, Janne and Vehmaan-Kreula,
Pirjo and Bartenstein, Peter and Brendel, Matthias and
Edbauer, Dieter and Lindner, Simon},
title = {{D}evelopment and {P}reclinical {E}valuation of a
{C}opper-64-{L}abeled {A}ntibody {T}argeting
{G}lycine-{A}lanine {D}ipeptides for {PET} {I}maging of
{C}9orf72-{A}ssociated {A}myotrophic {L}ateral
{S}clerosis/{F}rontotemporal {D}ementia},
journal = {ACS pharmacology $\&$ translational science},
volume = {7},
number = {5},
issn = {2575-9108},
address = {Washington, DC},
publisher = {ACS Publications},
reportid = {DZNE-2024-00568},
pages = {1404 - 1414},
year = {2024},
abstract = {Aggregating poly(glycine-alanine) (poly-GA) is derived from
the unconventional translation of the pathogenic intronic
hexanucleotide repeat expansion in the C9orf72 gene, which
is the most common genetic cause of frontotemporal dementia
(FTD) and amyotrophic lateral sclerosis (ALS). Poly-GA
accumulates predominantly in neuronal cytoplasmic inclusions
unique to C9orf72 ALS/FTD patients. Poly-GA is, therefore, a
promising target for PET/CT imaging of FTD/ALS to monitor
disease progression and therapeutic interventions. A novel
64Cu-labeled anti-GA antibody (mAb1A12) targeting the
poly-GA protein was developed and evaluated in a transgenic
mouse model. It was obtained with high radiochemical purity
(RCP), radiochemical yield (RCY), and specific activity, and
showed high stability in vitro and ex vivo and specifically
bound to poly-GA. The affinity of NODAGA-mAb1A12 for poly-GA
was not affected by this modification.
[64Cu]Cu-NODAGA-mAb1A12 was injected into transgenic mice
expressing GFP-(GA)175 in excitatory neurons driven by
Camk2a-Cre and in control littermates. PET/CT imaging was
performed at 2, 20, and 40 h post-injection (p.i.) and
revealed a higher accumulation in the cortex in transgenic
mice than in wild-type mice, as reflected by higher
standardized uptake value ratios (SUVR) using the cerebellum
as the reference region. The organs were isolated for
biodistribution and ex vivo autoradiography. Autoradiography
revealed a higher cortex-to-cerebellum ratio in the
transgenic mice than in the controls. Results from
autoradiography were validated by immunohistochemistry and
poly-GA immunoassays. Moreover, we confirmed antibody uptake
in the CNS in a pharmacokinetic study of the perfused
tissues. In summary, [64Cu]Cu-NODAGA-mAb1A12 demonstrated
favorable in vitro characteristics and an increased relative
binding in poly-GA transgenic mice compared to wild-type
mice in vivo. Our results with this first-in-class
radiotracer suggested that targeting poly-GA is a promising
approach for PET/CT imaging in FTD/ALS.},
cin = {AG Edbauer / AG Haass / AG Zhou},
ddc = {610},
cid = {I:(DE-2719)1110004 / I:(DE-2719)1110007 /
I:(DE-2719)5000080},
pnm = {352 - Disease Mechanisms (POF4-352)},
pid = {G:(DE-HGF)POF4-352},
typ = {PUB:(DE-HGF)16},
pmc = {pmc:PMC11091963},
pubmed = {pmid:38751620},
doi = {10.1021/acsptsci.4c00037},
url = {https://pub.dzne.de/record/269527},
}