Kazan Federal University Digital Repository

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

Show simple item record

dc.contributor.author Fujiki K.
dc.contributor.author Kanayama Y.
dc.contributor.author Yano S.
dc.contributor.author Sato N.
dc.contributor.author Yokokita T.
dc.contributor.author Ahmadi P.
dc.contributor.author Watanabe Y.
dc.contributor.author Haba H.
dc.contributor.author Tanaka K.
dc.date.accessioned 2020-01-15T22:12:06Z
dc.date.available 2020-01-15T22:12:06Z
dc.date.issued 2019
dc.identifier.issn 2041-6520
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/157019
dc.description.abstract © The Royal Society of Chemistry. α-Emission radiotherapeutics has potential to be one of most effective cancer therapeutics. Herein, we report a facile synthesis of an 211 At-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 211 At. 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 211 At produced in the cyclotron at the RIKEN Nishina Center, at which highly radioactive 211 At can be produced, readily furnished the 211 At-labeled trastuzumab with a maximum specific activity of 15 MBq μg −1 and retention of the native binding affinity. Intratumor injection of the 211 At-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.
dc.relation.ispartofseries Chemical Science
dc.title <sup>211</sup> At-labeled immunoconjugate via a one-pot three-component double click strategy: practical access to α-emission cancer radiotherapeutics
dc.type Article
dc.relation.ispartofseries-issue 7
dc.relation.ispartofseries-volume 10
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 1936
dc.source.id SCOPUS20416520-2019-10-7-SID85061597495


Files in this item

This item appears in the following Collection(s)

  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

Show simple item record

Search DSpace


Advanced Search

Browse

My Account

Statistics