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Issue 116, 2015
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Trivalent Gd-DOTA reagents for modification of proteins

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Abstract

The development of novel protein-targeted MRI contrast agents crucially depends on the ability to derivatise suitable targeting moieties with a high payload of relaxation enhancer (e.g., gadolinium(III) complexes such as Gd-DOTA), without losing affinity for the target proteins. Here, we report robust synthetic procedures for the preparation of trivalent Gd-DOTA reagents with various chemical handles for site-specific modification of biomolecules. The reagents were shown to successfully label proteins through isothiocyanate ligation or through site-specific thiol–maleimide ligation and strain-promoted azide–alkyne cycloaddition.

Graphical abstract: Trivalent Gd-DOTA reagents for modification of proteins

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Publication details

The article was received on 01 Oct 2015, accepted on 29 Oct 2015 and first published on 02 Nov 2015


Article type: Paper
DOI: 10.1039/C5RA20359G
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Citation: RSC Adv., 2015,5, 96194-96200
  • Open access: Creative Commons BY license
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    Trivalent Gd-DOTA reagents for modification of proteins

    M. J. Fisher, D. J. Williamson, G. M. Burslem, J. P. Plante, I. W. Manfield, C. Tiede, J. R. Ault, P. G. Stockley, S. Plein, A. Maqbool, D. C. Tomlinson, R. Foster, S. L. Warriner and R. S. Bon, RSC Adv., 2015, 5, 96194
    DOI: 10.1039/C5RA20359G

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