Evaluation of Astatine-211-Labeled Fibroblast Activation Protein Inhibitor (FAPI): Comparison of Different Linkers with Polyethylene Glycol and Piperazine
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- Ayaka Aso
- Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Hinako Nabetani
- Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Yoshifumi Matsuura
- Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Yuichiro Kadonaga
- Department of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, 2-2 Yamadaoka, Suita 565-0871, Osaka, Japan
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- Yoshifumi Shirakami
- Division of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Tadashi Watabe
- Department of Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, 2-2 Yamadaoka, Suita 565-0871, Osaka, Japan
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- Taku Yoshiya
- Peptide Institute, Inc., 7-2-9 Saito-asagi, Ibaraki 567-0085, Osaka, Japan
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- Masayoshi Mochizuki
- Peptide Institute, Inc., 7-2-9 Saito-asagi, Ibaraki 567-0085, Osaka, Japan
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- Kazuhiro Ooe
- Radioisotope Research Center, Institute for Radiation Sciences, Osaka University, 2-4 Yamadaoka, Suita 565-0871, Osaka, Japan
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- Atsuko Kawakami
- Research Center for Ultra-High Voltage Electron Microscopy, Osaka University, 7-1 Mihogaoka, Ibaraki 567-0047, Osaka, Japan
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- Naoya Jinno
- R&D Division, Alpha Fusion Inc., 10-1 Mihogaoka, Ibaraki 567-0047, Osaka, Japan
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- Atsushi Toyoshima
- Division of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Hiromitsu Haba
- RIKEN Nishina Center for Accelerator-Based Science, 2-1 Hirosawa, Wako 351-0198, Saitama, Japan
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- Yang Wang
- RIKEN Nishina Center for Accelerator-Based Science, 2-1 Hirosawa, Wako 351-0198, Saitama, Japan
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- Jens Cardinale
- Department of Nuclear Medicine, University Hospital Düsseldorf, Moorenstr. 5, 40225 Düsseldorf, Germany
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- Frederik Lars Giesel
- Division of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Atsushi Shimoyama
- Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Kazuko Kaneda-Nakashima
- Division of Science, Institute for Radiation Sciences, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
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- Koichi Fukase
- Department of Chemistry, Graduate School of Science, Osaka University, 1-1 Machikaneyama, Toyonaka 560-0043, Osaka, Japan
書誌事項
- 公開日
- 2023-05-12
- 資源種別
- journal article
- 権利情報
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- https://creativecommons.org/licenses/by/4.0/
- DOI
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- 10.3390/ijms24108701
- 公開者
- MDPI AG
説明
<jats:p>Fibroblast activation proteins (FAP) are overexpressed in the tumor stroma and have received attention as target molecules for radionuclide therapy. The FAP inhibitor (FAPI) is used as a probe to deliver nuclides to cancer tissues. In this study, we designed and synthesized four novel 211At-FAPI(s) possessing polyethylene glycol (PEG) linkers between the FAP-targeting and 211At-attaching moieties. 211At-FAPI(s) and piperazine (PIP) linker FAPI exhibited distinct FAP selectivity and uptake in FAPII-overexpressing HEK293 cells and the lung cancer cell line A549. The complexity of the PEG linker did not significantly affect selectivity. The efficiencies of both linkers were almost the same. Comparing the two nuclides, 211At was superior to 131I in tumor accumulation. In the mouse model, the antitumor effects of the PEG and PIP linkers were almost the same. Most of the currently synthesized FAPI(s) contain PIP linkers; however, in our study, we found that PEG linkers exhibit equivalent performance. If the PIP linker is inconvenient, a PEG linker is expected to be an alternative.</jats:p>
収録刊行物
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- International Journal of Molecular Sciences
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International Journal of Molecular Sciences 24 (10), 8701-, 2023-05-12
MDPI AG
