Severin S E, Shmyrev I I, Posypanova G A, Sologub V K, Nakachian R, Andreani J, Severin E S
Moscow's Research Institute of Medical Ecology, Russia.
Biochem Mol Biol Int. 1995 Oct;37(2):385-92.
An oncofetal protein, human alpha-fetoprotein, was selected as a vector molecule for targeted delivery of antitumor substances. Conjugates of alpha-fetoprotein with doxorubicin, daunomycin, calichemicin, carboxyphosphamide, bleomycetin, chlorbutin, cis-platinum, methotrexate were synthesized. All conjugates displayed a highly selective antitumor cytotoxic activity towards human cell cultures. The optimal alpha-fetoprotein:cytotoxic compound ratio was shown to be 1:3 - 1:5. The results obtained serve as a basis for creating antitumor preparations of a new generation, which are highly selective to tumor cells owing to receptor-mediated endocytosis.
一种癌胚蛋白，即人甲胎蛋白，被选作靶向递送抗肿瘤物质的载体分子。合成了甲胎蛋白与阿霉素、柔红霉素、刺孢霉素、羧磷酰胺、博来霉素、氯布替诺、顺铂、甲氨蝶呤的缀合物。所有缀合物对人细胞培养物均表现出高度选择性的抗肿瘤细胞毒性活性。结果表明，甲胎蛋白与细胞毒性化合物的最佳比例为1:3至1:5。所获得的结果为制备新一代抗肿瘤制剂奠定了基础，这些制剂由于受体介导的内吞作用而对肿瘤细胞具有高度选择性。
