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疾病相关的药物靶标蛋白与小分子化合物的亲和作用研究是当今新药研发的热点领域,基于靶蛋白与配体亲和作用的筛选技术已成为与基于靶蛋白活性高通量筛选技术高度互补的药物先导化合物发现关键技术。本文综述了亲和质谱技术用于筛选和检测指定靶蛋白的小分子配体的基本原理和主要优势,详细介绍了该技术应用于大规模化合物库筛选、分子片段库筛选、天然产物粗提物筛选和蛋白质与胞内代谢物相互作用研究领域的主要进展。
Disease-related drug target protein and small molecule compounds affinity research is a hot area of new drug research and development, based on the target protein and ligand affinity screening technology has become highly efficient and based on the target protein activity of high-throughput screening technology is highly complementary Drug lead compounds found key technologies. This review summarizes the basic principles and major advantages of affinity mass spectrometry for the screening and detection of small molecule ligands for a given target protein. The application of this technique in large-scale screening of compound libraries, molecular fragment library screening, crude extract of natural products Screening and major advances in the field of protein-intracellular metabolite interactions.