Method for the Rapid Screening of Drug Candidates Using Single‐Protein Tracking in a Living Cell,Bulletin of the Korean Chemical Society

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Method for the Rapid Screening of Drug Candidates Using Single‐Protein Tracking in a Living Cell
Bulletin of the Korean Chemical Society ( IF 2.3 ) Pub Date : 2020-12-28 , DOI: 10.1002/bkcs.12198
Dong‐Kyun Kim ₁ , Young Sook Kim ₂ , Chan Sik Kim ₃ , Nam Ki Lee ₄

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Screening drug candidates rapidly is the first step for developing new pharmaceutical drugs. One of the most promising ways to reduce the number of screening steps and cost is to directly use living cells for screening instead of using purified target proteins. Compounds screened using living cells will have increased biological activity compared to those screened with in vitro assays. Here, we report a robust method for screening drug candidates in living cells based on single‐protein imaging. We employed single‐protein tracking to observe the variation in the diffusion coefficient of membrane proteins treated with the candidate compounds. The diffusion coefficient shift was introduced as a criterion for selecting the potential candidate compounds. We tested three different membrane proteins, epidermal growth factor receptor, ErbB2, and ErbB3, and found effective natural compounds for each protein. The screening method we introduce will be widely used for screening potential drug candidates using living cells.

中文翻译：

在活细胞中使用单蛋白追踪快速筛选候选药物的方法

快速筛选候选药物是开发新药物的第一步。减少筛选步骤数量和成本的最有前途的方法之一是直接使用活细胞进行筛选，而不是使用纯化的靶蛋白。与体外筛选的化合物相比，使用活细胞筛选的化合物具有更高的生物学活性分析。在这里，我们报告了一种基于单蛋白成像筛选活细胞中候选药物的可靠方法。我们采用单蛋白跟踪来观察用候选化合物处理的膜蛋白扩散系数的变化。引入扩散系数偏移作为选择潜在候选化合物的标准。我们测试了三种不同的膜蛋白，表皮生长因子受体，ErbB2和ErbB3，并发现每种蛋白有效的天然化合物。我们介绍的筛选方法将被广泛用于利用活细胞筛选潜在的候选药物。

更新日期：2020-12-28

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