Journal Article

PUBDB-2026-01409

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Fluorine‐18‐Labeled Nucleotide Analogs Targeting Ecto‐5'‐Nucleotidase (CD73) for Positron Emission Tomography Imaging of Solid Tumors

Dobelmann, C. ; Schmies, C. C. ; Rolshoven, G. W. ; Scortichini, M. ; Wagner, S. ; Isaak, A. ; Idris, R. M. ; Dabel, J. ; Grey, L. ; Losenkova, K. ; Moschütz, S. ; Hroub, H. A. ; Keim, A. ; Höppner, S. ; Sandholm, J. ; Boström, P. ; Hollmén, M. ; Sträter, N. ; Hermann, S. ; Yegutkin, G. G. ; Jacobson, K. A. ; Schelhaas, S. ; Müller, C. E. (Corresponding author) ; Junker, A. (Corresponding author)

2026
Wiley-VCH Weinheim

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Please use a persistent id in citations: doi:10.1002/ange.202522758  doi:10.3204/PUBDB-2026-01409

Abstract: Ecto-5’-nucleotidase (CD73) is a potential new drug target for cancer immunotherapy. Its overexpression is associated with various aggressive cancers, including triple-negative breast cancer (TNBC) and pancreatic cancer, making it a promising target for diagnostic imaging. Besides antibodies, small-molecule CD73 inhibitors have been developed and are currently in clinical trials. This study aimed to develop and evaluate fluorine-18 labeled high-affinity CD73 inhibitors as tracers for the non-invasive positron emission tomography (PET) imaging of CD73 expression in cancer. Two CD73 inhibitors were selected for radiolabeling based on their high potency (Ki values of ca. 1 nM) and favorable pharmacokinetic properties, yielding [18F]PSB-19427 ([18F]1) and [18F]MRS-4648 ([18F]2). Ex vivo imaging studies on human breast cancer tissues indicated specific binding of both radiotracers. Subsequent in vivo studies proved [18F]1 to be superior due to its long elimination half-life and its accumulation in TNBC and pancreatic cancer tissues, suggesting its potential as a versatile PET tracer for imaging of various solid tumors. Compared to [18F]FDG, [18F]1 was superior in visualizing TNBC, offering potential advantages over [18F]FDG in terms of specificity and diagnostic accuracy. Thus, [18F]1 is a PET tracer with outstanding properties suitable for broad application in cancer diagnosis and personalized medicine.

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Contributing Institute(s):

1. EMBL-User (EMBL-User)

Research Program(s):

1. 6G3 - PETRA III (DESY) (POF4-6G3) (POF4-6G3)
2. GRK 1328 - GRK 1328: Gehirn und Verhalten: Neurobiologische Grundlagen von Emotion und sozialer Kognition bei Schizophrenie und Autismus (13820592) (13820592)
3. GRK 2873 - GRK 2873: Werkzeuge und Wirkstoffe der Zukunft - Innovative Methoden und neue Modalitäten in der Medizinischen Chemie (494832089) (494832089)

Experiment(s):

1. PETRA Beamline P14 (PETRA III)
2. PETRA Beamline P13 (PETRA III)

Appears in the scientific report 2026

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Database coverage:
; ; ; DEAL Wiley ; Ebsco Academic Search ; Nationallizenz ; SCOPUS

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