Novel chemoselective 18F-radiolabeling of thiol-containing biomolecules under mild aqueous conditions

Aristeidis Chiotellis; Filippo Sladojevich; Linjing Mu; Adrienne Müller Herde; Ibai E. Valverde; Vladimir Tolmachev; Roger Schibli; Simon M. Ametamey; Thomas L. Mindt

doi:10.1039/C6CC01982J

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Novel chemoselective ¹⁸F-radiolabeling of thiol-containing biomolecules under mild aqueous conditions†

Aristeidis Chiotellis,^a Filippo Sladojevich,^a Linjing Mu,^a Adrienne Müller Herde,^a Ibai E. Valverde,^b Vladimir Tolmachev,

^c Roger Schibli,^a Simon M. Ametamey^a and Thomas L. Mindt*^abd

Author affiliations

* Corresponding authors

^a Center for Radiopharmaceutical Sciences ETH-PSI-USZ, Institute of Pharmaceutical Sciences ETH, Vladimir-Prelog Weg 4, CH-8093 Zurich, Switzerland
E-mail: t.mindt@gmx.ch

^b Division of Radiopharmaceutical Chemistry, University of Basel Hospital, Petersgraben 4, CH-4031 Basel, Switzerland

^c Department of Immunology, Genetics and Pathology, Medical Radiation Science Program, Rudbeck Laboratory, Uppsala University, SE-75181 Uppsala, Sweden

^d Ludwig Boltzmann Institute for Applied Diagnostics, General Hospital of Vienna, Währinger Gürtel 18-20, A-1090 Vienna, Austria

Abstract

We report a novel prosthetic group based on a heterocyclic methylsulfone derivative for the rapid, stable, and chemoselective ¹⁸F-labeling of thiol-containing (bio)molecules under mild aqueous reaction conditions. Compared to established maleimide approaches, the new methodology displays some clear advantages for imaging probe development.

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Article information

DOI: https://doi.org/10.1039/C6CC01982J
Article type: Communication
Submitted: 05 Mar 2016
Accepted: 30 Mar 2016
First published: 30 Mar 2016

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Chem. Commun., 2016,52, 6083-6086

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Novel chemoselective ¹⁸F-radiolabeling of thiol-containing biomolecules under mild aqueous conditions

A. Chiotellis, F. Sladojevich, L. Mu, A. Müller Herde, I. E. Valverde, V. Tolmachev, R. Schibli, S. M. Ametamey and T. L. Mindt, Chem. Commun., 2016, 52, 6083 DOI: 10.1039/C6CC01982J

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