Harper Jay, Mao Shenlan, Strout Patrick, Kamal Adeela
Oncology Research, MedImmune Inc., Gaithersburg, MD, USA.
Methods Mol Biol. 2013;1045:41-9. doi: 10.1007/978-1-62703-541-5_3.
Antibody-drug conjugates (ADCs) combine the selectivity of a monoclonal antibody with the killing potency of a cytotoxic drug. For an antibody to function as a successful component of an ADC, it needs to bind to the target antigen on the surface of tumor cells and then be internalized by the cell. Following internalization, the ADC has to be transported to the lysosome where subsequent intracellular processing of the ADC will release the biologically active drug to exert its cytotoxic effects on tumor cells. This chapter describes some of the techniques that are currently used to determine internalization and proper intracellular trafficking of antibodies in order to select an optimal antibody for ADC therapeutics.
抗体药物偶联物（ADC）将单克隆抗体的选择性与细胞毒性药物的杀伤效力结合在一起。要使抗体成功作为ADC的一个组成部分发挥作用，它需要与肿瘤细胞表面的靶抗原结合，然后被细胞内化。内化后，ADC必须被转运到溶酶体，在那里ADC随后的细胞内加工过程将释放出生物活性药物，以对肿瘤细胞发挥其细胞毒性作用。本章描述了一些目前用于确定抗体的内化和正确的细胞内转运的技术，以便为ADC治疗选择最佳抗体。
