Modulation of Protein-Protein Interactions for the Development of Novel Therapeutics.
Modulation of Protein-Protein Interactions for the Development of Novel Therapeutics.
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DOI：
10.1038/mt.2015.214
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发表时间：
2016-04
期刊：
影响因子：
--
通讯作者：
De Bosscher K
中科院分区：
文献类型：
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作者：
Petta I;Lievens S;Libert C;Tavernier J;De Bosscher K
蛋白质-蛋白质相互作用（PPIs）是大多数生物过程的基础。由于需要为一系列具有高度未满足医疗需求的疾病寻找新的治疗靶点，人们越来越有兴趣研究PPIs在药物发现中的未开发潜力。迄今为止，小分子抑制PPI是最常被探索的机制，导致药物开发取得重大进展。然而，PPI企稳也在逐渐取得进展。在这篇综述中，我们提供了一些PPIs的重点概述，这些PPIs控制着关键的调控途径，并构成了新疗法设计的靶点。我们讨论了已经在临床试验中进行的ppi调节小分子。此外，我们回顾了一些仍处于临床前研究阶段的ppi，但初步数据支持它们作为治疗靶点。
Protein–protein interactions (PPIs) underlie most biological processes. An increasing interest to investigate the unexplored potential of PPIs in drug discovery is driven by the need to find novel therapeutic targets for a whole range of diseases with a high unmet medical need. To date, PPI inhibition with small molecules is the mechanism that has most often been explored, resulting in significant progress towards drug development. However, also PPI stabilization is gradually gaining ground. In this review, we provide a focused overview of a number of PPIs that control critical regulatory pathways and constitute targets for the design of novel therapeutics. We discuss PPI-modulating small molecules that are already pursued in clinical trials. In addition, we review a number of PPIs that are still under preclinical investigation but for which preliminary data support their use as therapeutic targets.