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Folate-mediated targeting of antineoplastic drags, imaging agents, and nucleic acids to cancer cells

机译:叶酸介导的抗肿瘤药,显像剂和核酸靶向癌细胞

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摘要

The receptor for the vitamin, folic acid, is overexpressed on a number of human tumors, including cancers of the ovary, kidney, uterus, testis, brain, colon, lung, and myelocytic blood cells. Conjugates of folic acid linked via its gamma-carboxyl to either a single drug molecule or assembly of molecules can bind to and enter receptor-expressing cancer cells via folate receptor-mediated endocytosis. Because the affinity of folate conjugates for cell surface folate receptors is high (K-D
机译:维生素叶酸的受体在许多人类肿瘤中过表达,包括卵巢癌,肾癌,子宫癌,睾丸癌,脑癌,结肠癌,肺癌和骨髓细胞癌。通过其γ-羧基连接到单个药物分子或分子组件的叶酸缀合物可以通过叶酸受体介导的内吞作用结合并进入表达受体的癌细胞。因为叶酸结合物对细胞表面叶酸受体的亲和力很高(​​KD <相似(KD类似于10(-10)M),所以叶酸衍生化可以在正常细胞存在的情况下选择性地将诊断剂和治疗剂传递给癌细胞。这篇综述将总结针对叶酸介导的蛋白质毒素,显像剂,反义寡脱氧核苷酸,基因和脂质体专门针对体外和体内癌细胞的研究(C)1998 Elsevier Science BV [参考文献:33]

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