N-[2-(maleimido)ethyl]-3-(trimethylstannyl)benzamide, a molecule for radiohalogenation of proteins and peptides. (February 2015)

• Record Type: Journal Article
• Authors: Aneheim, Emma; Foreman, Mark R. StJ.; Jensen, Holger; Lindegren, Sture
• Is Part Of: Applied radiation and isotopes. Volume 96(2015:Feb.)
• Page Start: 1
• Page End: 5
• Publication Date: 2015-02
• Subjects: Halogenation -- Astatine-211 -- Site specific antibody labelling -- Peptide labelling -- Targeted radiotherapy -- Electrophilic aromatic substitution; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2014.11.007
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: 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 125 I and 211 At, indicating potential use within targeted radiotherapy. Highlights: A novel conjugation agent for radiohalogenation of proteins and peptides was synthesized. The characterized agent is N-[2-(maleimido)ethyl]-3-(trimethylstannyl)benzamide. The conjugation agent was halogenated with bromine, iodine ( 125 I) and 211 At.