% 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{Hoffmann:1046742,
      author       = {Hoffmann, Chris and Gröner, Benedikt and Bahutski, Victor
                      and Endepols, Heike and Lindemeyer, Johannes and Saniternik,
                      Sven and Drewes, Birte and Timmer, Marco and Gokhadze, Otari
                      and Brugger, Melanie and Neumaier, Felix and Neumaier, Bernd
                      and Zlatopolskiy, Boris D.},
      title        = {{C}omparative evaluation of three 18{F}-fluorinated {FAP}
                      ligands in rodent tumor models},
      journal      = {European journal of medicinal chemistry},
      volume       = {299},
      issn         = {0009-4374},
      address      = {Amsterdam [u.a.]},
      publisher    = {Elsevier Science},
      reportid     = {FZJ-2025-03941},
      pages        = {118103},
      year         = {2025},
      note         = {This work was supported by Deutsche Forschungsgemeinschaft
                      (DFG; grant number ZL 65/4-1), the Shota Rustaveli National
                      Science Foundation of Georgia (SRNSFG; grant number
                      JFZ–II–22-074), and the Excellent Research Support
                      Program, University of Cologne (UoC) Forum 2023 (Multimodal
                      Preclinical Imaging Platform University Cologne [MUPIC]).},
      abstract     = {Fibroblast activation protein (FAP) is almost exclusively
                      expressed on cancer-associated stromal cells, making it
                      apromising target for tumor imaging by positron emission
                      tomography (PET). While 68Ga- or Al[18F]F-labeled
                      FAPinhibitors (FAPIs) have been characterized in detail, the
                      potential advantages of FAPIs containing a covalentlybound
                      18F-label remain largely unknown. The aim of the present
                      work was to address this gap by comparing twoFAPIs with a
                      covalently bound 18F-label and the chelator-based
                      radioligand Al[18F]F-FAPI-42.The 18F-labeled FAPIs were
                      prepared by direct (6-[18F]F-FAPI) or indirect
                      ([18F]AFA-FAPI) radiofluorination,or by the Al[18F]F
                      chelation method (Al[18F]F-FAPI-42), which afforded the
                      tracers in activity yields of 11–57 $\%and$ with molar
                      activities of 5–170 GBq/μmol. Cellular uptake studies
                      revealed significantly higher accumulationof all three
                      candidates in HT1080-FAP compared to HT1080-WT cells.
                      6-[18F]F-FAPI and Al[18F]F-FAPI-42showed comparable
                      FAP-selectivity and tumor uptake in mice inoculated with the
                      two cell lines and rats bearingsubcutaneous DSL-6A/C1
                      tumors, while no in vivo FAP-selectivity was observed for
                      [18F]AFA-FAPI. Al[18F]FFAPI-42 exhibited lower hepatobiliary
                      excretion and faster clearance from FAP-negative tissues in
                      the subcutaneoustumor models. In contrast, 6-[18F]F-FAPI
                      showed higher tumor uptake and better tumor retention in
                      anintracerebral U87 glioma tumor model. When compared to the
                      established glioma tracer [18F]FET, both FAPtargetingtracers
                      visualized intracerebral tumors with more than two-fold
                      higher tumor-to-background ratios.In conclusion, while the
                      chelator-based radioligand Al[18F]F-FAPI-42 is well-suited
                      for visualization of peripheraltumors, 6-[18F]F-FAPI with a
                      covalently bound 18F-label shows more favorable properties
                      for braintumor imaging.},
      cin          = {INM-5},
      ddc          = {610},
      cid          = {I:(DE-Juel1)INM-5-20090406},
      pnm          = {5253 - Neuroimaging (POF4-525)},
      pid          = {G:(DE-HGF)POF4-5253},
      typ          = {PUB:(DE-HGF)16},
      doi          = {10.1016/j.ejmech.2025.118103},
      url          = {https://juser.fz-juelich.de/record/1046742},
}