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Protein-protein interactions as drug targets

机译:蛋白质-蛋白质相互作用作为药物靶标

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摘要

Modulation of protein-protein interactions (PPIs) is becoming increasingly important in drug discovery and chemical biology. While a few years ago this target class' was deemed to be largely undruggable an impressing number of publications and success stories now show that targeting PPIs with small, drug-like molecules indeed is a feasible approach. Here, we summarize the current state of small-molecule inhibition and stabilization of PPIs and review the active molecules from a structural and medicinal chemistry angle, especially focusing on the key examples of iNOS, LFA-1 and 14-3-3.
机译:在药物发现和化学生物学中,蛋白质间相互作用(PPI)的调节变得越来越重要。几年前,这一目标类别被认为是相当难以捉摸的,令人印象深刻的出版物和成功案例现在都表明,以药物样小分子靶向PPI确实是一种可行的方法。在这里,我们总结了小分子抑制和稳定PPI的现状,并从结构和药物化学的角度回顾了活性分子,特别是重点关注了iNOS,LFA-1和14-3-3的关键实例。

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