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

作者：Fletcher Sally A; Sin Pak Kwan Brian; Nobles Muriel; Arstad Erik; Tinker Andrew; Baker James R^*

来源：Organic and Biomolecular Chemistry, 2015, 13(37): 9559-9563.

DOI：10.1039/c5ob01468a

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.

• 出版日期2015