Development of a stable radioiodinating reagent to label monoclonal antibodies for radiotherapy of cancer.
Development of a stable radioiodinating reagent to label monoclonal antibodies for radiotherapy of cancer.
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发表时间：
1989-02
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影响因子：
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通讯作者：
D. Wilbur;S. W. Hadley;Mark D. Hylandes;P. Abrams;P. Beaumier;A. Morgan;J. Reno;A. Fritzberg
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文献类型：
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作者：
D. Wilbur;S. W. Hadley;Mark D. Hylandes;P. Abrams;P. Beaumier;A. Morgan;J. Reno;A. Fritzberg
已经研究了放射性碘标记单克隆抗体的方法，使得标记的抗体不经历体内脱碘。该方法利用琥珀酰亚胺基对碘苯甲酸酯与抗体的缀合。碘苯甲酸酯通过使用有机金属中间体进行放射性标记以促进反应。因此，琥珀酰亚胺基对-三-正丁基甲锡烷基苯甲酸酯以60-90%的放射化学产率进行放射性标记，随后以80-90%的产率与抗体偶联。用该方法标记的两种单独的抗黑色素瘤抗体（9.2.27和NR-M1-05）进行动物生物分布研究，并在携带人黑色素瘤异种移植物的裸鼠中进行检查。当碘苯甲酰基标记的抗体与使用氯胺-T放射性碘标记法标记的相同抗体进行比较时，在小鼠的甲状腺和胃中观察到放射性定位存在非常大的差异。在放射性碘标记抗体的组织分布中几乎没有其他显著差异。
A method of radioiodinating monoclonal antibodies such that the labeled antibodies do not undergo in vivo deiodination has been studied. The method utilizes conjugation of succinimidyl para-iodobenzoate to the antibody. The iodobenzoate was radiolabeled by using an organometallic intermediate to facilitate the reaction. Thus, succinimidyl para-tri-n-butylstannylbenzoate was radiolabeled in 60-90% radiochemical yield and subsequently conjugated to the antibody in 80-90% yield. Animal biodistribution studies were carried out with two separate anti-melanoma antibodies (9.2.27 and NR-M1-05) labeled by this method, and examined in nude mice bearing human melanoma tumor xenografts. Very large differences in the localization of radioactivity were observed in the thyroids and stomachs of mice when the iodobenzoyl-labeled antibodies were compared with the same antibodies labeled using the chloramine-T method of radioiodination. Few other significant differences in the tissue distribution of the radioiodinated antibodies were seen.