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- W4297519327 abstract "The alpha-emitting radioisotope astatine-211 (211At) is a potential candidate for targeted alpha therapy. For low toxic astatination of FAPI(s) with dihydroxyboryl group (B-FAPI), a dihydroxyboryl-astatine substitution reaction was developed without using any toxic reagents. We achieved efficient astatination with less than 10 µg of B-FAPI, which is feasible in drug manufacturing conditions. Additionally, the FAPα selectivity and cell uptake of 211At-labeled FAPI(s) (211At-FAPI) exhibited promising results for high antitumor efficacy. Alpha-emitting radioisotope Astatine-211 (211At) is a potential candidate for targeted alpha therapy. For astatination of FAPI(s) with dihydroxyboryl group (B-FAPI), a dihydroxyboryl-astatine substitution reaction was developed without any toxic reagents. We achieved efficient astatination with less than 10 µg of B-FAPI, which is feasible in drug manufacturing conditions. Additionally, the FAPα selectivity and cell-uptake of 211At-labeled FAPI(s) exhibited promising results." @default.
- W4297519327 created "2022-09-29" @default.
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- W4297519327 date "2022-11-05" @default.
- W4297519327 modified "2023-10-17" @default.
- W4297519327 title "Substrate Study for Dihydroxyboryl Astatine Substitution Reaction with Fibroblast Activation Protein Inhibitor (FAPI)" @default.
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- W4297519327 doi "https://doi.org/10.1246/cl.220391" @default.
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