摘要/Abstract
天然产物是创新药物的重要来源,确定活性天然产物的靶标蛋白和作用机制是新药开发的关键.在本篇综述中,对近二十年来在活性天然产物靶标鉴定领域出现的新技术和新方法进行简要的回顾和总结,通过实例重点介绍化学蛋白质组学和生物物理学方法在天然产物靶标蛋白鉴定方面的应用,讨论各种策略的优势和不足,并对其适用范围,应用前景和发展趋势作了前瞻性的展望.
关键词: 天然产物, 靶标鉴定, 化学蛋白质组学, 生物物理学, 表型筛选
Natural products are rich sources of drugs for the treatment of human diseases, while identification of the protein targets and mode of actions is one of the most significant and challenging steps in drug discovery across bioactive natural products. This review describes recent progresses in the methodology of target identification of natural products, highlights examples of target identification utilizing chemical proteomics and biophysical strategies, and discusses the advantages, limitations, applications, and challenges of each strategy.
Key words: natural products, target identification, chemical proteomics, biophysics, phenotype screening
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