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生物活性小分子靶标的明确鉴定需要整合多种分析方法,从多层次、多角度阐明其作用靶标的有效性和专属性。即使这样也都无法排除假阳性或者假阴性的产生,只有各种方法联用才能有力阐明小分子的生物活性与相应靶标。本文系统综述了生物活性小分子靶标鉴定与验证的方法,总结为直接法(包括生物素亲和标签、亲和胶、噬菌体展示、光交联法、亲和磁珠法等)和间接法(包括药物亲和反应靶标分析、蛋白质组学分析、化学基因组学分析和代谢组学分析等)两种。每种方法分别列举了1个实例,并讨论了其优势和劣势,以明确其适用范围和应用前景。
The clear identification of bioactive small molecule targets requires the integration of multiple analytical methods to elucidate the effectiveness and specificity of their targets of action at multiple levels and from multiple perspectives. Even though this can not be ruled out false positive or false negative, only a variety of methods can effectively elucidate the biological activity of small molecules and the corresponding target. This review summarizes the methods for the identification and verification of bioactive small molecule targets, including the direct method (including biotinylated affinity tag, affinity gel, phage display, photocrosslinking method, affinity bead method, etc.) and indirect method Including drug affinity reaction target analysis, proteomics analysis, chemical genomics analysis and metabonomics analysis). Each method cited an example respectively, and discussed its advantages and disadvantages to clarify its scope and application prospects.