N-12-(maleimido)ethyl]-3-(trimethylstannyl)benzamide, a molecule for radiohalogenation of proteins and peptides

作者：Aneheim Emma^*; Foreman Mark R StJ; Jensen Holger; Lindegren Sture

来源：Applied Radiation and Isotopes, 2015, 96: 1-5.

DOI：10.1016/j.apradiso.2014.11.007

• Halogenation
• Astatine-211
• Site specific antibody labelling
• Peptide labelling
• Targeted radiotherapy
• Electrophilic aromatic substitution

In this work a new coupling reagent, N[2-(maleimido)ethyl]-3-(trimethylstannyl)benzamide, for radiohalogenation has been synthesized and characterized. The reagent is intended to either be attached to reduced disulfide bridges of proteins (making the halogenation site-specific) or to free terminal cysteine groups on peptides. The new reagent was also shown to be easily halogenated with inactive bromine and iodine as well as I-125 and At-211, indicating potential use within targeted radiotherapy.

• 出版日期2015-2