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@ARTICLE{Zlatopolskiy:863491,
author = {Zlatopolskiy, Boris and Endepols, Heike and Krapf, Philipp
and Guliyev, Mehrab and Urusova, Elizaveta A. and Richarz,
Raphael and Hohberg, Melanie and Dietlein, Markus and
Drzezga, Alexander and Neumaier, Bernd},
title = {{D}iscovery of 18{F}-{JK}-{PSMA}-7, a {PET} {P}robe for the
{D}etection of {S}mall {PSMA}-{P}ositive {L}esions},
journal = {Journal of nuclear medicine},
volume = {60},
number = {6},
issn = {2159-662X},
address = {New York, NY},
publisher = {Soc.},
reportid = {FZJ-2019-03545},
pages = {817 - 823},
year = {2019},
abstract = {Prostate specific membrane antigen (PSMA) expressed by the
vast majority of prostate cancers (PCa) is a promising
target for PCa imaging. The application of PSMA specific
18F-labeled PET probes like 18F-DCFPyL and 18F-PSMA-1007
considerably improved the accuracy of PCa tumor detection.
However, there remains a need for further improvements
regarding sensitivity and specificity. The aim of this study
was the development of highly selective and specific PSMA
probes with enhanced imaging properties, in comparison with
18F-DCFPyL, 18F-PSMA-1007 and 68Ga-PSMA-11. Methods: Eight
novel 18F-labeled PSMA ligands were prepared. Their cellular
uptake in PSMA+ LNCaP C4-2 and PSMA– PC-3 cells was
compared to that of 18F-DCFPyL. The most promising
candidates were additionally evaluated by µPET in healthy
rats using PSMA+ peripheral ganglia as a model for small PCa
lesions. PET images of the ligand with the best outcome,
18F-JK-PSMA-7, were compared to those of 18F-DCFPyL,
18F-PSMA-1007 and 68GaPSMA-11 with respect to key image
quality parameters for the time frame 60-120 min. Results:
Compared to 18F-DCFPyL, 18F-JK-PSMA-7 demonstrated increased
PSMA specific cellular uptake. While target-to-background
ratios of 18F-DCFPyL and 18F-PSMA-1007 were comparable, this
parameter was higher for 18F-JK-PSMA-7 and lower for
68Ga-PSMA-11. Image acutance was significantly higher for
18F-JK-PSMA-7 and 18F-PSMA-1007 compared to 18F-DCFPyL and
68Ga-PSMA-11. Image resolution was similar for all four
tracers. 18F-PSMA-1007 demonstrated significantly higher
blood protein binding and bone uptake than the other
tracers. Conclusion: 18F-JK-PSMA-7 is a promising candidate
for high quality visualization of small PSMA-positive
lesions. Excellent preclinical imaging properties justify
further preclinical and clinical studies of this tracer.},
cin = {INM-5 / INM-2},
ddc = {610},
cid = {I:(DE-Juel1)INM-5-20090406 / I:(DE-Juel1)INM-2-20090406},
pnm = {572 - (Dys-)function and Plasticity (POF3-572)},
pid = {G:(DE-HGF)POF3-572},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:30389823},
UT = {WOS:000470084400029},
doi = {10.2967/jnumed.118.218495},
url = {https://juser.fz-juelich.de/record/863491},
}