在N-琥珀酰亚胺基3-（三甲基锡基）苯甲酸酯标记中使用N-碘代琥珀酰亚胺作为氧化剂对抗体进行高效砹化。

High-efficiency astatination of antibodies using N-iodosuccinimide as the oxidising agent in labelling of N-succinimidyl 3-(trimethylstannyl)benzoate.

作者信息

Lindegren S, Andersson H, Bäck T, Jacobsson L, Karlsson B, Skarnemark G

机构信息

Department of Radiation Physics, Göteborg University, Sahlgrenska University Hospital, SE-413 45, Göteborg, Sweden.

出版信息

Nucl Med Biol. 2001 Jan;28(1):33-9. doi: 10.1016/s0969-8051(00)00171-2.

DOI:10.1016/s0969-8051(00)00171-2

PMID:11182562

Abstract

Monoclonal antibodies C215, reactive with colorectal carcinomas, and MOv18, reactive with most of the ovarian carcinomas, were radiohalogenated with [211At]astatine. The radiohalogen was conjugate coupled to antibodies via the intermediate labelling reagent N-succinimidyl-3-(trimethylstannyl)benzoate (m-MeATE) in a two-step, single-pot reaction. Optimisation of the labelling of the reagent was achieved using N-iodosuccinimide, NIS, as the oxidising agent. The yields ranged from 69-95% in the labelling of 0.1-1.0 nmole of the m-MeATE precursor. Subsequent conjugation to antibodies resulted in yields of 58+/-7%. In vitro binding to tumour cells showed that the immunoreactivity of both antibodies was retained after astatine labelling.

摘要

与结肠直肠癌反应的单克隆抗体C215和与大多数卵巢癌反应的MOv18，用[211At]砹进行放射性卤化。放射性卤素通过中间标记试剂N-琥珀酰亚胺基-3-(三甲基锡基)苯甲酸酯(m-MeATE)在两步单罐反应中与抗体共轭偶联。使用N-碘代琥珀酰亚胺(NIS)作为氧化剂实现了试剂标记的优化。在标记0.1-1.0纳摩尔m-MeATE前体时，产率范围为69-95%。随后与抗体共轭的产率为58±7%。体外与肿瘤细胞的结合表明，砹标记后两种抗体的免疫反应性均得以保留。