Otsuji E, Yamaguchi T, Yata Y, Nishi H, Okamoto K, Taniguchi K, Kato M, Kotani T, Yamaoka N, Kitamura K
First Department of Surgery, Kyoto Prefectural University of Medicine, Japan.
J Surg Oncol. 1994 Dec;57(4):230-4. doi: 10.1002/jso.2930570405.
The anticancer agent neocarzinostatin (NCS) was bound covalently to human/mouse chimeric Fab fragments of the monoclonal antibody A7 to form the conjugate chA7Fab-NCS. The antitumor effect of chA7Fab-NCS was tested by measuring the inhibition of 3H-thymidine incorporation into human pancreatic carcinoma cells. The chA7Fab-NCS was approximately 2.3 times as effective as free NCS against human pancreatic carcinoma cells which reacted with the monoclonal antibody A7. The antitumor activity of chA7Fab-NCS was inhibited by excess chA7Fab. ChA7Fab-NCS had an antitumor effect equivalent to free NCS on human pancreatic carcinoma cells which did not react with the monoclonal antibody A7. ChA7Fab-NCS appears to be a potentially useful conjugate for immunotargeting chemotherapy against pancreatic carcinoma.
抗癌药物新制癌菌素（NCS）与单克隆抗体A7的人/鼠嵌合Fab片段共价结合，形成偶联物chA7Fab-NCS。通过测量3H-胸腺嘧啶核苷掺入人胰腺癌细胞的抑制率来测试chA7Fab-NCS的抗肿瘤效果。对于与单克隆抗体A7反应的人胰腺癌细胞，chA7Fab-NCS的有效性约为游离NCS的2.3倍。过量的chA7Fab可抑制chA7Fab-NCS的抗肿瘤活性。对于不与单克隆抗体A7反应的人胰腺癌细胞，chA7Fab-NCS具有与游离NCS相当的抗肿瘤效果。chA7Fab-NCS似乎是一种潜在有用的用于胰腺癌免疫靶向化疗的偶联物。
