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Issue 37, 2015
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A dual optical and nuclear imaging reagent for peptide labelling via disulfide bridging

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Abstract

We report a concise approach to a multimodal imaging reagent for peptide labelling via disulfide bridging. The reagent is constructed using a one pot, three component, [3 + 2] cycloaddition of a fluorescent azide with a dithiomaleimide-alkyne, with concomitant incorporation of 125I. The dithiomaleimide handle then enables site selective conjugation to a disulfide bond of a peptide whilst retaining the key structural bridging functionality, as exemplified on the therapeutic peptide octreotide.

Graphical abstract: A dual optical and nuclear imaging reagent for peptide labelling via disulfide bridging

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Publication details

The article was received on 17 Jul 2015, accepted on 17 Aug 2015 and first published on 24 Aug 2015


Article type: Communication
DOI: 10.1039/C5OB01468A
Author version available: Download Author version (PDF)
Citation: Org. Biomol. Chem., 2015,13, 9559-9563
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    A dual optical and nuclear imaging reagent for peptide labelling via disulfide bridging

    S. A. Fletcher, P. K. B. Sin, M. Nobles, E. Årstad, A. Tinker and J. R. Baker, Org. Biomol. Chem., 2015, 13, 9559
    DOI: 10.1039/C5OB01468A

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