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Issue 7, 2019
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211At-labeled immunoconjugate via a one-pot three-component double click strategy: practical access to α-emission cancer radiotherapeutics

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Abstract

α-Emission radiotherapeutics has potential to be one of most effective cancer therapeutics. Herein, we report a facile synthesis of an 211At-labeled immunoconjugate for use as an α-emission molecular targeting therapy. We synthesized a tetrazine probe modified with closo-decaborate(2-), a prosthetic group that forms a bioavailable stable complex with 211At. Our one-pot three-component double-click labeling method was used to attach decaborate to trastuzumab (anti-HER2 antibody) using decaborate-tetrazine and TCO-aldehyde probes without reducing the antibody binding affinity. Labeling the decaborate-attached trastuzumab with 211At produced in the cyclotron at the RIKEN Nishina Center, at which highly radioactive 211At can be produced, readily furnished the 211At-labeled trastuzumab with a maximum specific activity of 15 MBq μg−1 and retention of the native binding affinity. Intratumor injection of the 211At-labeled trastuzumab in BALB/c nude mice implanted with HER2-expressing epidermoid cancer cells yielded efficient accumulation at the targeted tumor site as well as effective suppression of tumor growth.

Graphical abstract: 211At-labeled immunoconjugate via a one-pot three-component double click strategy: practical access to α-emission cancer radiotherapeutics

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Publication details

The article was received on 25 Oct 2018, accepted on 19 Dec 2018 and first published on 21 Dec 2018


Article type: Edge Article
DOI: 10.1039/C8SC04747B
Citation: Chem. Sci., 2019,10, 1936-1944
  • Open access: Creative Commons BY license
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    211At-labeled immunoconjugate via a one-pot three-component double click strategy: practical access to α-emission cancer radiotherapeutics

    K. Fujiki, Y. Kanayama, S. Yano, N. Sato, T. Yokokita, P. Ahmadi, Y. Watanabe, H. Haba and K. Tanaka, Chem. Sci., 2019, 10, 1936
    DOI: 10.1039/C8SC04747B

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