基于流式细胞术受体占位实验设计的研究现状

Current situation of receptor occupancy assays design based on flow cytometry

受体占位(RO)是评价药物与受体结合的重要研究内容,可用于药效学和安全性评估,在药物研发的各个阶段均发挥重要作用,但该研究也面临许多技术和操作可行性方面的挑战。建立一个准确的可重复的RO方法需考虑诸多因素,如:选择合适的检测模式(直接法或间接法)、检测试剂、样品类型和目标细胞群等,还要充分考虑受体表达、受体调节以及样本稳定性等其他因素对实验结果的影响。本文对基于流式细胞术受体占位实验设计的几个关键考虑要点进行了系统全面地讨论。

Receptor occupancy(RO)is an important research content for the evaluation of drug-receptor binding.RO can be used to assess pharmacodynamics and safety,and plays an important role in all stages of drug development.But the research also faces many challenges in technical and operational feasibility.There are many factors to be considered when establishing an accurate and repeatable RO method,such as selecting appropriate detection mode(direct or indirect method),detection reagents,sample type and target cell population,etc.The effects of receptor expression and receptor regulation as well as sample stability on the measure results should be fully considered.In this paper,a systematic and comprehensive discussion of several key considerations for receptor occupancy experiment designs based on flow cytometry is presented.