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New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone–cycloalkyne click reaction

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Abstract

We report the first pretargeting in vivo study using the Strain-Promoted Sydnone–Alkyne Cycloaadition (SPSAC) reaction. The injection of a fluorine-18 labeled cyclooctyne three days after cetuximab bearing chlorosydnone moieties allowed a significant detection of the tumor by PET imaging suggesting an efficient click reaction inside the tumoral site. With a kinetic constant superior to 300 M−1 s−1, the SPSAC reaction might be an interesting tool, in addition to tetrazine-cyclooctene ligation, for in vivo chemistry.

Graphical abstract: New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone–cycloalkyne click reaction

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Publication details

The article was received on 16 Jul 2019, accepted on 01 Aug 2019 and first published on 02 Aug 2019


Article type: Communication
DOI: 10.1039/C9CC05486C
Chem. Commun., 2019, Advance Article

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    New fluorine-18 pretargeting PET imaging by bioorthogonal chlorosydnone–cycloalkyne click reaction

    M. Richard, C. Truillet, V. L. Tran, H. Liu, K. Porte, D. Audisio, M. Roche, B. Jego, S. Cholet, F. Fenaille, B. Kuhnast, F. Taran and S. Specklin, Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9CC05486C

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