抗表皮生长因子受体单克隆抗体LA22与抗肿瘤抗生素丝裂霉素C的偶联物对裸鼠人肿瘤异种移植生长的抑制作用
Inhibition of human tumor xenograft growth in nude mice by a conjugate of monoclonal antibody LA22 to epidermal growth factor receptor with anti-tumor antibiotics mitomycin C.
作者信息
Shao Wei, Zhao Shan, Liu Zhaofei, Zhang Jianzhong, Ma Shujun, Sato J Denry, Zhang Peng, Tong Mei, Han Jiping, Wang Yan, Bai Dongmei, Wang Fan, Sun Le
机构信息
Welson Pharmaceuticals, Inc., 10239 Threadneedle CT, Ellicott City, MD 21042, USA.
出版信息
Biochem Biophys Res Commun. 2006 Oct 20;349(2):816-24. doi: 10.1016/j.bbrc.2006.08.114. Epub 2006 Aug 28.
Anti-EGFR monoclonal antibodies LA22 and Erbitux bind to different epitopes of EGFR. The chemimmunoconjugates of MMC with LA22 or Erbitux were prepared, and in vitro cytotoxicity assays with A549 cells showed that LA22-MMC was much more potent than Erbitux or Erbitux-MMC. Viabilities of A549 cells treated with LA22-MMC, Erbitux or Erbitux-MMC were 35%, 94%, and 81%, respectively. Immunoscintigraphy of xenografts of human A431 and A549 cells in nude mice both showed that (125)I-labeled-LA22-MMC enriched in tumor sites prominently. Most importantly, in vivo assays showed LA22-MMC was significantly more effective than free drug MMC in the treatment of subcutaneous xenografts of human A431 cells in nude mice (83% inhibition for LA22-MMC and 30% for MMC). We concluded that LA22-MMC could be a very potent drug for treatment of solid tumors.
抗表皮生长因子受体（EGFR）单克隆抗体LA22和爱必妥（Erbitux）与EGFR的不同表位结合。制备了丝裂霉素（MMC）与LA22或爱必妥的化学免疫偶联物，对A549细胞进行的体外细胞毒性试验表明，LA22-MMC比爱必妥或爱必妥-MMC的效力要强得多。用LA22-MMC、爱必妥或爱必妥-MMC处理的A549细胞的活力分别为35%、94%和81%。对裸鼠体内人A431和A549细胞异种移植瘤进行免疫闪烁显像，结果均显示（125）I标记的LA22-MMC在肿瘤部位显著富集。最重要的是，体内试验表明，在治疗裸鼠体内人A431细胞皮下异种移植瘤方面，LA22-MMC比游离药物MMC显著有效得多（LA22-MMC的抑制率为83%，MMC为30%）。我们得出结论，LA22-MMC可能是一种治疗实体瘤的强效药物。
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