Human TfR1 was universal y expressed in dif erent tissues. The major function of TfR1 was to facilitate delivery of transferrin across cells and blood-brain barrier (BBB). As a result, iron homo-stasis was maintained. TfR1 was recognised as a critical target for tumor and brain disease therapy due to its over expression in tumor cells and BBB. In recent years, drug carriers based on TfR1 recognition were developed such as Transferrin (Tf), anti-TfR1 antibody and TfR1 binding peptide. These carriers bind to TfR1 specifical y and enter into cellor BBB through receptor mediated endocytosis. Chemicals conjugated with these carriers can be facilitated to enter into tumor cells and brain tissue. Therapeutic proteins can be engineered to fused with anti-TfR1 antibody and transported across BBB.%人转铁蛋白受体（TfR1)在不同组织器官中普遍表达，其主要功能是协助转铁蛋白在细胞和血脑屏障内外转运，维持细胞铁平衡。在肿瘤细胞中以及血脑屏障中，TfR1的表达水平明显高于正常细胞组织，因此，TfR1被认为是肿瘤靶向治疗和脑部疾病靶向治疗的重要靶点。基于TfR1靶向治疗的药物载体主要有转铁蛋白（Tf）、抗TfR1抗体、TfR1结合肽，这些生物大分子能与TfR1特异性结合，结合之后可以通过受体介导的跨胞转运机制进入细胞或穿过血脑屏障。将小分子药与这些载体偶联可以促进许多亲水性的化疗药物或神经治疗药物进入肿瘤细胞或血脑屏障，而许多中枢神经治疗性大分子则主要通过融合蛋白的方式与抗TfR1抗体连接转运进入中枢神经系统。
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