% IMPORTANT: The following is UTF-8 encoded. This means that in the presence
% of non-ASCII characters, it will not work with BibTeX 0.99 or older.
% Instead, you should use an up-to-date BibTeX implementation like “bibtex8” or
% “biber”.
@ARTICLE{Eder:179273,
author = {A.-C. Eder$^*$ and J. Matthias and M. Schäfer$^*$ and J.
Geberlein$^*$ and N. Steinacker$^*$ and U. Bauder-Wüst$^*$
and L.-C. Domogalla$^*$ and M. Roscher$^*$ and U.
Haberkorn$^*$ and M. Eder$^*$ and K. Kopka$^*$},
title = {{A} {N}ew {C}lass of {PSMA}-617-{B}ased {H}ybrid
{M}olecules for {P}reoperative {I}maging and
{I}ntraoperative {F}luorescence {N}avigation of {P}rostate
{C}ancer.},
journal = {Pharmaceuticals},
volume = {15},
number = {3},
issn = {1424-8247},
address = {Basel},
publisher = {MDPI},
reportid = {DKFZ-2022-00555},
pages = {267},
year = {2022},
abstract = {The development of PSMA-targeting low-molecular-weight
hybrid molecules aims at advancing preoperative imaging and
accurate intraoperative fluorescence guidance for improved
diagnosis and therapy of prostate cancer. In hybrid probe
design, the major challenge is the introduction of a bulky
dye to peptidomimetic core structures without affecting
tumor-targeting properties and pharmacokinetic profiles.
This study developed a novel class of PSMA-targeting hybrid
molecules based on the clinically established theranostic
agent PSMA-617. The fluorescent dye-bearing candidates of
the strategically designed molecule library were evaluated
in in vitro assays based on their PSMA-binding affinity and
internalization properties to identify the most favorable
hybrid molecule composition for the installation of a bulky
dye. The library's best candidate was realized with
IRDye800CW providing the lead compound.
Glu-urea-Lys-2-Nal-Chx-Lys(IRDye800CW)-DOTA (PSMA-927) was
investigated in an in vivo proof-of-concept study, with
compelling performance in organ distribution studies,
PET/MRI and optical imaging, and with a strong PSMA-specific
tumor uptake comparable to that of PSMA-617. This study
provides valuable insights about the design of
PSMA-targeting low-molecular-weight hybrid molecules, which
enable further advances in the field of peptidomimetic
hybrid molecule development.},
keywords = {PSMA (Other) / guided surgery (Other) / hybrid molecules
(Other) / prostate cancer (Other) / theranostics (Other)},
cin = {E030 / FR01 / E060 / DD01},
ddc = {610},
cid = {I:(DE-He78)E030-20160331 / I:(DE-He78)FR01-20160331 /
I:(DE-He78)E060-20160331 / I:(DE-He78)DD01-20160331},
pnm = {315 - Bildgebung und Radioonkologie (POF4-315)},
pid = {G:(DE-HGF)POF4-315},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:35337061},
pmc = {pmc:PMC8954540},
doi = {10.3390/ph15030267},
url = {https://inrepo02.dkfz.de/record/179273},
}