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A yeast two-hybrid system for the screening and characterization of small-molecule inhibitors of protein–protein interactions identifies a novel putative Mdm2-binding site in p53

机译:用于筛选和表征蛋白质相互作用的小分子抑制剂的酵母双杂交系统在p53中鉴定出一个新的推测的Mdm2结合位点

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摘要

BackgroundProtein–protein interactions (PPIs) are fundamental to the growth and survival of cells and serve as excellent targets to develop inhibitors of biological processes such as host-pathogen interactions and cancer cell proliferation. However, isolation of PPI inhibitors is extremely challenging. While several in vitro assays to screen for PPI inhibitors are available, they are often expensive, cumbersome, and require large amounts of purified protein. In contrast, limited in vivo assays are available to screen for small-molecule inhibitors of PPI.
机译:背景蛋白质-蛋白质相互作用(PPI)是细胞生长和存活的基础,并且是开发生物过程抑制剂(例如宿主-病原体相互作用和癌细胞增殖)的绝佳靶标。然而,PPI抑制剂的分离极具挑战性。尽管有几种用于筛选PPI抑制剂的体外测定方法可用,但它们通常很昂贵,麻烦且需要大量的纯化蛋白。相反,有限的体内分析可用于筛选PPI的小分子抑制剂。

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