Goldenberg D M, Sharkey R M, Primus F J, Mizusawa E, Hawthorne M F
Proc Natl Acad Sci U S A. 1984 Jan;81(2):560-3. doi: 10.1073/pnas.81.2.560.
Antibody against carcinoembryonic antigen (CEA) was conjugated with p-[1,2-dicarba-closo-[1-3H]do-decaboran(12)-2-yl] benzenediazonium ion by an azo-coupling reaction, resulting in 30 boron atoms per IgG molecule with no loss of antibody protein. Antibody immunoreactivity was not appreciably affected by this conjugation and was stable after incubation in vitro in hamster plasma for 24 hr. The efficacy of the boron-conjugated anti-CEA IgG for localizing selectively in CEA-containing human colonic carcinomas propagated in the hind leg musculature of hamsters was evaluated by labeling the antibodies with 131I and determining distribution of the radioactivity in vivo. The results show that the boron-conjugated antibodies retain selective localization in the tumors, thus indicating their suitability for transporting boron-10 to tumors for use in neutron-capture therapy of cancer.
通过偶氮偶联反应,将癌胚抗原(CEA)抗体与对-[1,2-二碳-闭式-[1-³H]十二硼烷(12)-2-基]苯重氮离子偶联,每个IgG分子产生30个硼原子,且抗体蛋白无损失。这种偶联对抗体免疫反应性没有明显影响,并且在仓鼠血浆中体外孵育24小时后仍保持稳定。通过用¹³¹I标记抗体并测定其在体内的放射性分布,评估了硼偶联抗CEA IgG在选择性定位在仓鼠后腿肌肉组织中生长的含CEA的人结肠癌中的功效。结果表明,硼偶联抗体在肿瘤中保留了选择性定位,从而表明它们适用于将硼-10转运至肿瘤用于癌症的中子俘获治疗。