抗体偶联药物内吞作用机制的研究进展

发布时间：2018-03-10 18:55

  本文选题：抗体偶联药物　切入点：内吞作用　出处：《中国新药杂志》2017年10期 　论文类型：期刊论文

【摘要】：抗体偶联药物(antibody-drug conjugate,ADC)由单克隆抗体和小分子细胞毒药物通过化学连接子连接,兼顾了单克隆抗体的选择性和小分子药物的细胞毒效力。ADC进入体内后,可通过单克隆抗体的靶向作用结合于肿瘤表面的靶抗原,经内吞作用进入细胞内,在溶酶体的化学或酶促作用下释放小分子细胞毒药物导致靶细胞死亡。ADC的内吞作用是ADC发挥药效的关键,并且已经成为ADC开发阶段的重要部分。由于缺乏对于ADC内吞作用的整体认识,目前对于内吞效率和内吞机制的研究方法开发存在着诸多挑战。本文对ADC的内吞机制、影响因素和研究方法等方面的进展进行了综合归纳和阐述。
[Abstract]:The antibody-drug conjugate drug (ADCC) was linked by monoclonal antibody and small molecular cytotoxic drug via chemical linker, which took into account the selectivity of monoclonal antibody and the cytotoxicity of small molecule drug. ADC entered the body. The target antigen that binds to the surface of the tumor through the targeting action of monoclonal antibody and enters the cell through endocytosis. The endocytosis of the target cell death caused by the release of small molecular cytotoxic drugs under the chemical or enzymatic action of lysosome is the key to the effect of ADC. And has become an important part of the ADC development stage. Due to the lack of overall understanding of the endocytosis of ADC, there are many challenges to the development of endocytosis efficiency and endocytosis mechanism. This paper discusses the endocytosis mechanism of ADC. The development of influencing factors and research methods are summarized and expounded.
【作者单位】： 中国药科大学江苏省药物代谢动力学重点实验室;天士力集团研究院药理毒理研究中心;
【分类号】：R945
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本文编号：1594629