抗体（Anti-Met Fab）-顺铂复合物的制备及其与DNA活性研究
Synthesize of CDDP-Met conjugates and the study of activity between CDDP-Met conjugates and DNA
nti-Met Fab是c-Met的特异性人源化抗体，能与肿瘤细胞膜上的Met胞外区特异性结合，并进入细胞内。顺铂是一种被广泛应用的抗肿瘤药物,其抗肿瘤机理缘于铂与DNA间较强的键合作用,顺铂能够与DNA片段同一链上相邻GG或GA的N7原子结合形成双功能复合物,从而造成DNA的变形、DNA复制转录机制的改变以及导致DNA信息程序化突变,进而引起细胞的凋亡。本文利用anti-Met Fab抗体作为载体，制备了抗体（Anti-Met Fab）-顺铂复合物(CDDP-Met复合物复合物)，每个anti-Met Fab 抗体可载4-7个顺铂分子。本文考察了该复合物在体外及细胞内与DNA 的相互作用。结果表明：Anti-Met Fab抗体修饰后的顺铂仍然保留了与DNA反应的活性。CDDP-Met复合物与HepG2的研究表明：修饰后的顺铂毒性降低。
Anti-Met Fab could recognize Met extracelluar domain in native conformation with relatively high affinity. Anti-Met Fab were able to be internalized into c-Met over-expressed tumor cell lines through binding to c-Met recptor.Cisplatin (cis-diamminedichloro-platinum(II))is one of the most commonly used and successful chemotherapeutic agents employed to date.The major cell-killing effect is due to cisplatin-DNA adducts.CDDP-Met conjugates was synthesized in the article，with 4-7CDDP/抗体. The reaction between CDDP-Met conjugates and DNA was carried out.The results indicated that CDDP-Met conjugates could react whit DNA as that of free CDDP. Also, cytotoxicity of CDDP-Met conjugates was lower compared to free DOX.
高启合、徐健、周倩、朱进、孙柏旺
药学基础医学生物化学
抗体复合物NA
nti-Met FabconjugatesNA
高启合,徐健,周倩,朱进,孙柏旺.抗体（Anti-Met Fab）-顺铂复合物的制备及其与DNA活性研究[EB/OL].(2011-03-14)[2025-08-11].http://www.paper.edu.cn/releasepaper/content/201103-555.点此复制
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