학술논문
Substrate Study for Dihydroxyboryl Astatine Substitution Reaction with Fibroblast Activation Protein Inhibitor (FAPI)
Document Type
Article
Author
Aso, Ayaka; Kaneda-Nakashima, Kazuko; Nabetani, Hinako; Kadonaga, Yuichiro; Shirakami, Yoshifumi; Watabe, Tadashi; Yoshiya, Taku; Mochizuki, Masayoshi; Koshino, Yuki; Ooe, Kazuhiro; Kawakami, Atsuko; Jinno, Naoya; Toyoshima, Atsushi; Haba, Hiromitsu; Wang, Yang; Cardinale, Jens; Giesel, Frederik L; Shimoyama, Atsushi; Fukase, Koichi
Source
Chemistry Letters; November 2022, Vol. 51 Issue: 11 p1091-1094, 4p
Subject
Language
ISSN
03667022; 13480715
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.