The membrane transferrin receptor-mediated endocytosis or internalization of the complex of transferrin bound iron and the transferrin receptor is the major route of cellular iron uptake. This efficient cellular uptake pathway has been exploited for the site-specific delivery not only of anticancer drugs and proteins, but also of therapeutic genes into proliferating malignant cells that overexpress the transferrin receptors. This is achieved either chemically by conjugation of transferrin with therapeutic drugs, proteins, or genetically by infusion of therapeutic peptides or proteins into the structure of transferrin. The resulting conjugates significantly improve the cytotoxicity and selectivity of the drugs. The coupling of DNA to transferrin via a polycation or liposome serves as a potential alternative to viral vector for gene therapy. Moreover, the OX26 monoclonal antibody against the rat transferrin receptor offers great promise in the delivery of therapeutic agents across the blood-brain barrier to the brain.

中文翻译：

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通过运铁蛋白受体介导的内吞途径靶向药物递送。

膜转铁蛋白受体介导的内吞作用或与转铁蛋白结合的铁与转铁蛋白受体的复合物的内在化是细胞摄取铁的主要途径。这种有效的细胞摄取途径已被用于不仅将抗癌药和蛋白质，而且还通过治疗基因将其特异地传递到过度表达运铁蛋白受体的恶性细胞中。这可以通过化学方法将转铁蛋白与治疗药物，蛋白质结合来实现，也可以通过将治疗性肽或蛋白质输注到转铁蛋白的结构中来实现。所得的缀合物显着改善了药物的细胞毒性和选择性。DNA通过聚阳离子或脂质体与运铁蛋白的偶联可作为病毒载体用于基因治疗的潜在替代方法。