利用设计的分子抑制α螺旋介导的蛋白质-蛋白质相互作用
利用设计的分子抑制α螺旋介导的蛋白质-蛋白质相互作用
Inhibition of α-helix-mediated protein–protein interactions using designed molecule
Inhibition of protein–protein interactions (PPIs) represents a significant challenge because it is unclear how they can be effectively and selectively targeted using small molecules. Achieving this goal is critical given the defining role of these interactions in biological processes. A rational approach to inhibitor design based on the secondary structure at the interface is the focus of much research, and different classes of designed ligands have emerged, some of which effectively and selectively disrupt targeted PPIs. This Review discusses the relevance of PPIs and, in particular, the importance of α-helix-mediated PPIs to chemical biology and drug discovery with a focus on designing inhibitors, including constrained peptides, foldamers and proteomimetic-derived ligands. In doing so, key challenges and major advances in developing generic approaches for the elaboration of PPI inhibitors are highlighted. The challenges faced in developing such ligands as drug leads — and how criteria applied to these may differ from conventional small-molecule drugs — are summarized.
蛋白之间是相互作用细胞信号传递的基础,干扰细胞蛋白之间的相互作用也是药物设计的一个重要靶点.如何合理设计呢?
好吧,让我们来学学这片 nature chemistry
不错的文章噢~~ 这篇和药物重定向的综述很不错，非常感谢！
页:
[1]