A high-affinity [(18) F]-labeled phosphoramidate peptidomimetic PSMA-targeted inhibitor for PET imaging of prostate cancer
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F86652036%3A_____%2F15%3A00450935" target="_blank" >RIV/86652036:_____/15:00450935 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.nucmedbio.2015.06.003" target="_blank" >http://dx.doi.org/10.1016/j.nucmedbio.2015.06.003</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.nucmedbio.2015.06.003" target="_blank" >10.1016/j.nucmedbio.2015.06.003</a>
Alternative languages
Result language
angličtina
Original language name
A high-affinity [(18) F]-labeled phosphoramidate peptidomimetic PSMA-targeted inhibitor for PET imaging of prostate cancer
Original language description
Introduction: In this study, a structurally modified phosphoramidate scaffold, with improved prostate-specific membrane antigen (PSMA) avidity, stability and in vivo characteristics, as a PET imaging agent for prostate cancer (PCa), was prepared and evaluated.Methods: p-Fluorobenzoyl-aminohexanoate and 2-(3-hydroxypropyl)glycine were introduced into the PSMA-targeting scaffold yielding phosphoramidate 5. X-ray crystallography was performed on the PSMA/5 complex. [F-18]5 was synthesized, and cell uptakeand internalization studies were conducted in PSMA(+) LNCaP and CWR22Rv1 cells and PSMA(-) PC-3 cells. In vivo PET imaging and biodistribution studies were performed at 1 and 4 h post injection in mice bearing CWR22Rv1 tumor, with or without blocking agent. Results: The crystallographic data showed interaction of the p-fluorobenzoyl group with an arene-binding cleft on the PSMA surface. In vitro studies revealed elevated uptake of [F-18]5 in PSMA(+) cells (2.2% in CWR22Rv1 and 12.1% in L
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
EB - Genetics and molecular biology
OECD FORD branch
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Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Nuclear Medicine and Biology
ISSN
0969-8051
e-ISSN
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Volume of the periodical
42
Issue of the periodical within the volume
10
Country of publishing house
US - UNITED STATES
Number of pages
8
Pages from-to
780-787
UT code for WoS article
000361423700004
EID of the result in the Scopus database
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