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

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, readi

SUBMITTER: Fujiki K 

PROVIDER: S-EPMC6385556 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature