药物活性成分靶标蛋白的鉴定研究进展
摘 要:活性成分与细胞内靶蛋白的相互作用,是药物发挥作用的基础。目前,对药物活性成分的鉴定主要分为两个途径。一方面是以小分子天然产物来筛选靶标蛋白,称作逆向策略(Reverse strategy),包括化学蛋白质组学(Chemical proteomics),化学基因组学(Chemical genetics)和生物物理学(Biophysics)等方法;另一方面可依据天然产物引起的组织或细胞表型变化或与之相关的信号通路和作用网络推测并确定天然产物的靶标,此方法称作正向策略(Forward strategy),主要包括差异基因组学,蛋白质组学分析,细胞形态分析等方法[1]。
关键词:靶标蛋白;活性基团;小分子探针;LC-MS
Identification of drug active component target protein
Abstract: The interaction between active components and intracellular target proteins is the basis of drug action. At present, the identification of drug active ingredients is mainly divided into two ways. On the one hand, target proteins are screened by natural products of small molecules, known as Reverse strategy, including Chemical proteomics, Chemical genetics and Biophysics. On the other hand, the target of natural products can be speculated and determined based on the tissue or cell phenotypic changes caused by natural products or the related signal pathways and action networks. This method is called Forward strategy and mainly includes differential genomics, proteomics analysis, cell morphology analysis and other methods [1].
Key words: target proteins; active group; Small molecule probe; LC-MS
1.逆向靶标鉴定策略
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