Aneheim Emma, Foreman Mark R StJ, Jensen Holger, Lindegren Sture
Targeted Alpha Therapy, Department of Radiation Physics, Sahlgrenska Academy at Gothenburg University, Gothenburg 41345, Sweden.
Nuclear Chemistry, Department of Chemical and Biological Engineering, Chalmers University of Technology, Gothenburg 41296, Sweden.
Appl Radiat Isot. 2015 Feb;96:1-5. doi: 10.1016/j.apradiso.2014.11.007. Epub 2014 Nov 11.
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.
在本研究中，已合成并表征了一种用于放射性卤化的新型偶联试剂N-[2-(马来酰亚胺基)乙基]-3-(三甲基锡基)苯甲酰胺。该试剂旨在连接到蛋白质的还原二硫键上（使卤化具有位点特异性）或连接到肽上的游离末端半胱氨酸基团上。新试剂还显示出易于用非活性溴和碘以及¹²⁵I和²¹¹At进行卤化，表明其在靶向放射治疗中有潜在用途。
