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Assays with Detection of Fluorescence Anisotropy: Challenges and Possibilities for Characterizing Ligand Binding to GPCRs
Trends in Pharmacological Sciences ( IF 13.8 ) Pub Date : 2017-11-01 , DOI: 10.1016/j.tips.2017.10.004
Ago Rinken , Darja Lavogina , Sergei Kopanchuk

Binding of fluorescent ligands (tracers) to their target receptors can be directly monitored over time, as the binding of a low-molecular-weight (LMW) tracer to a larger particle causes an increase of fluorescence anisotropy (FA). The combination of bright fluorophores, tracers with low nonspecific binding, and budded baculovirus particles (BVPs) for overexpression of G protein-coupled receptors (GPCRs) ensures a high signal-to-noise ratio in FA assays. The obtained data enable quantitative assessment of equilibrium binding and kinetic parameters for both the tracer and competing compounds as well as an estimation of the receptor concentration. FA assays have clear potential for implementation in drug screening systems, but also in studies of ligand-binding mechanisms for particular GPCRs.



中文翻译:

检测荧光各向异性的试验:表征配体与GPCR结合的挑战和可能性

随着时间的流逝,可以直接监测荧光配体(示踪剂)与其靶受体的结合,因为低分子量(LMW)示踪剂与较大颗粒的结合会导致荧光各向异性(FA)的增加。明亮的荧光团,具有低非特异性结合的示踪剂和芽状杆状病毒颗粒(BVP)结合使用,可过度表达G蛋白偶联受体(GPCR),可确保FA分析中的信噪比高。获得的数据能够定量评估示踪剂和竞争化合物的平衡结合和动力学参数,以及估算受体浓度。FA分析具有在药物筛选系统中实施以及在特定GPCR配体结合机制研究中的明显潜力。

更新日期:2017-11-01
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