Trivalent Gd-DOTA reagents for modification of proteins.

نویسندگان

  • Martin J Fisher
  • Daniel J Williamson
  • George M Burslem
  • Jeffrey P Plante
  • Iain W Manfield
  • Christian Tiede
  • James R Ault
  • Peter G Stockley
  • Sven Plein
  • Azhar Maqbool
  • Darren C Tomlinson
  • Richard Foster
  • Stuart L Warriner
  • Robin S Bon
چکیده

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.

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عنوان ژورنال:
  • RSC advances

دوره 5 116  شماره 

صفحات  -

تاریخ انتشار 2015