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叶酸受体α与肿瘤靶向治疗

  • 张琴 瞿爱东
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  • 200052 上海生物制品研究所有限责任公司第一研究室

网络出版日期: 2025-08-16

Folate receptor α and targeted therapy for tumors

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  • No.1 Research Laboratory, Shanghai Institute of Biological Products Co., Ltd., Shanghai 200052, China

Online published: 2025-08-16

摘要

 叶酸受体α(folate receptor α, FRα)是一种通过糖基磷脂酰肌醇锚定于细胞膜表面的单链糖蛋白,能够结合并转运叶酸到细胞内,而叶酸对于DNA合成、修复以及细胞代谢有着重要的作用。FRα在正常组织中限制性表达,但在上皮来源肿瘤组织中过度表达,并且表达量随肿瘤的进展而增高,因此可以作为治疗相关肿瘤的靶点。与叶酸结合的药物或者其他物质能够通过FRα介导的胞吞作用进入细胞发挥作用。靶向叶酸受体的单克隆抗体在肿瘤的诊断和治疗中也具有很好的前景。FRα的特异性组织表达可使单克隆抗体将细胞毒性物质送入肿瘤细胞而非正常组织,从而发挥杀伤肿瘤细胞或者抑制肿瘤进展的作用。

本文引用格式

张琴 瞿爱东 . 叶酸受体α与肿瘤靶向治疗[J]. 国际生物制品学杂志, 2015 , 38(5) : 250 -253 . DOI: 10.3760/cma.j.issn.1673-4211.2015.05.010

Abstract

 Folate receptor α (FRα) is a single-chain glycophosphatidylinositol- anchored protein on the cell surface, which binds folate and transports it into cells. Folate is a basic component of cell metabolism as well as DNA synthesis and repair. FRα is overexpressed in specific malignant tumors of epithelial origin while restrictively expressed in normal cells, and its expression level increases with tumor progression. Thus, FRα has been selected as a target and marker for cancer therapy. Various therapeutic agents linked to folate can then enter cancer cells via FRα-mediated endocytosis. Monoclonal antibodies targeting folate receptors have also shown potential in cancer diagnosis and therapy. The tissue-specific expression of FRα enables selective delivery of cytotoxic agents by monoclonal antibodies into malignant cells rather than normal tissues for killing tumor cells or preventing tumor progression.
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