受体-配体结合的质谱分析方法研究进展

Research Progress in Receptor Binding Assay by Mass Spectrometry

目的阐述受体-配体结合分析是一种重要的药物筛选方法,它通过体外实验来考察配体(药物)与受体的结合能力,在药物结构设计与新药筛选中发挥重要作用。方法查阅近期国内外相关文献。结果与结论质谱结合分析(MS binding assay)是近年来备受关注的一种受体-配体结合分析方法,该方法建立在质谱分析非放射性标记的配体的基础上,操作方便,灵敏度高,特异性好,适用范围广,样品用量少,克服了传统受体-配体结合分析中放射性标记和荧光标记的缺陷,是质谱技术在药物发现中的又一个新贡献。

OBJECTIVE To explain that receptor-ligand binding assay is an important drug screening method, which can quickly and inexpensively study the interactions between the targeted receptor and the potential ligands in vitro and provide information about the relative binding affinity of ligand-receptor. METHODS The correlative literature and abroad were collected and analyzed. RESULTS AND CONCLUSION The concept of MS binding assay based on mass spectrometric quantification of nonlabeled markers represents a promising alternative to conventional radioligands binding without inherent drawbacks. The technique will play an important role in the design and screening of receptor-targeting pharmaceuticals.