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叶酸受体介导的小分子抗肿瘤药物研究进展 被引量：5

Progress in folate receptor-mediated anticancer agent delivery
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摘要 靶向肿瘤细胞的药物研发近年来受到了极大的关注,除了阻断细胞信号通路的蛋白激酶抑制剂外,叶酸受体介导的药物释放也引起了研究者的广泛注意。叶酸受体在大多数人体肿瘤细胞中高度表达,而在正常细胞中很少表达或不表达。叶酸可以通过叶酸受体介导的内吞作用进入细胞,这为药物选择性释放提供了很好的途径。本文对近些年来基于叶酸受体介导的药物作用机制、设计策略,以及研发的叶酸-抗肿瘤药物缀合物进行综述,并介绍了该领域临床研究取得的最新进展。 Cancer therapies that exploit targeting ligands to deliver attached cytotoxic drugs selectively to ma- lignant cells are currently receiving significant attention. The folate receptor（FR） is a confirmed tumor-asso- ciated antigen that binds folate and folate-drug conjugates with very high affinity and shuttles these bound molecules inside cells via an endocytic mechanism. With the use of proper linkers and cleavable bond,small molecular weight, highly potent anticancer drugs can be released inside the cancer cells where they can per- form their desired cytotoxic functions. This review summarizes published activity data of various conjugates and highlights some newly emerging data from novel compounds which are currently under clinical investi- gation.
作者 付利强 丁实 杨玉社
机构地区 新药研究国家重点实验室中国科学院上海药物研究所
出处 《中国药物化学杂志》 CAS CSCD 2013年第3期226-234,共9页 Chinese Journal of Medicinal Chemistry
关键词 叶酸受体 内吞作用 叶酸缀合物 抗肿瘤药物 folate receptor endocytosis folate conjugate anticancer drug
分类号 R96 [医药卫生—药理学]
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参考文献37

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同被引文献42

  • 1杨晓葵,邢辉,郑芳,高庆蕾,王薇,卢运萍,马丁.凋亡相关基因和半胱天冬氨酸蛋白酶-3在卵巢癌顺铂耐药细胞株中的表达[J].中华妇产科杂志,2003,38(3):158-161. 被引量：7
  • 2赵斌,葛金芳,朱娟娟,黄晓晖,李俊.小议在MTT法测细胞增殖抑制率中IC_(50)的计算方法[J].安徽医药,2007,11(9):834-836. 被引量：165
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  • 8Hattinger CM, Stoico G, Michelacci F, et al. Mechanisms of gene amplification and evidence of eoamplifieation in drug-resistant human osteosarcoma cell lines[J]. Genes Chromosomes Cancer, 2009, 48(4):289-309.
  • 9Hagner N, Joerger M. Cancer chemotherapy: targeting folic acid synthesis[J]. Cancer Manag Res, 2010, 2:293-301.
  • 10Li L, Luan Y, Li X, et al. Dmnonstration of differential gene expression between sensitive and resistant ovarian tumor cells by fluorescence differential display-PCR analysis[J]. Oncol Rep, 2005, 13(5):793-799.

引证文献5

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中国药物化学杂志
2013年 第3期

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