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| Hauptseite > Publikationsdatenbank > Comparative evaluation of three 18F-fluorinated FAP ligands in rodent tumor models > print |
| Hauptseite > Publikationsdatenbank > Comparative evaluation of three 18F-fluorinated FAP ligands in rodent tumor models > print |
| 001 | 1046742 | ||
| 005 | 20251006201536.0 | ||
| 024 | 7 | _ | |a 10.1016/j.ejmech.2025.118103 |2 doi |
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| 037 | _ | _ | |a FZJ-2025-03941 |
| 082 | _ | _ | |a 610 |
| 100 | 1 | _ | |a Hoffmann, Chris |0 P:(DE-Juel1)180770 |b 0 |u fzj |
| 245 | _ | _ | |a Comparative evaluation of three 18F-fluorinated FAP ligands in rodent tumor models |
| 260 | _ | _ | |a Amsterdam [u.a.] |c 2025 |b Elsevier Science |
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| 500 | _ | _ | |a 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]). |
| 520 | _ | _ | |a 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. |
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| 773 | _ | _ | |a 10.1016/j.ejmech.2025.118103 |g Vol. 299, p. 118103 - |0 PERI:(DE-600)2005170-0 |p 118103 |t European journal of medicinal chemistry |v 299 |y 2025 |x 0009-4374 |
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