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Best practices for optimization and validation of flow cytometry‐based receptor occupancy assays
Cytometry Part B: Clinical Cytometry ( IF 3.4 ) Pub Date : 2020-12-01 , DOI: 10.1002/cyto.b.21970
Ed Hilt 1 , Yongliang S Sun 1 , Thomas W McCloskey 2 , Steve Eck 3 , Thomas McIntosh 4 , Katharine D Grugan 5 , David F Lanham 6 , Nathan Standifer 7 , Cherie Green 8 , Virginia Litwin 9 , Jennifer J Stewart 10
Affiliation  

In the development of therapeutic compounds that bind cell surface molecules, it is critical to demonstrate the extent to which the drug engages its target. For cell‐associated targets, flow cytometry is well‐suited to monitor drug‐to‐target engagement through receptor occupancy assays (ROA). The technology allows for the identification of specific cell subsets within heterogeneous populations and the detection of nonabundant cellular antigens. There are numerous challenges in the design, development, and implementation of robust ROA. Among the most difficult challenges are situations where there is receptor modulation or when the target‐antigen is expressed at low levels. When the therapeutic molecules are bi‐specific and bind multiple targets, these challenges are increased. This manuscript discusses the challenges and proposes best practices for designing, optimizing, and validating ROA.

中文翻译:

优化和验证基于流式细胞仪的受体占据检测的最佳实践

在开发与细胞表面分子结合的治疗性化合物时,证明药物与其靶标结合的程度至关重要。对于细胞相关靶点,流式细胞术非常适合通过受体占据测定 (ROA) 监测药物与靶点的结合。该技术可以识别异质群体中的特定细胞亚群并检测非丰富的细胞抗原。在稳健的 ROA 的设计、开发和实施中存在许多挑战。最困难的挑战是存在受体调节或靶抗原以低水平表达的情况。当治疗分子具有双特异性并结合多个靶标时,这些挑战就会增加。
更新日期:2021-01-21
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