蛋白质-蛋白质相互作用及其抑制剂研究进展

蛋白质-蛋白质相互作用在细胞活动和生命过程中扮演着非常重要的角色。基因调节、免疫应答、信号转导、细胞组装等等都离不开蛋白质-蛋白质的相互作用。近几年,靶向蛋白质-蛋白质相互作用及其抑制剂研究也逐渐成为研究的热点;但是蛋白质复合物相互作用界面的一些特点和性质,如相互作用界面较大、结合界面较为平坦等,使蛋白质-蛋白质相互作用及其抑制剂研究充满了挑战。本文主要总结了蛋白质-蛋白质相互作用界面的一些性质和特点,分析了界面特性与其抑制剂设计的关系,并讨论了蛋白质-蛋白质相互作用的理论预测方法及其抑制剂的类型和特点,最后又通过实例说明了如何进行蛋白质-蛋白质相互作用抑制剂的设计。

Research progress in protein-protein interactions and their inhibitors

Protein-protein interactions play important roles in a wide range of biological processes. Gene regulation, immune response, signal transduction, cellular architecture and many other mechanisms of cellular control are involved in the interactions of protein and protein. So the discovery of drugs that could prohibit protein-protein interactions has become a very active research field in recent years. However, it is full of challenge to design such inhibitors because of the unique properties of the protein-protein interfaces. For example, the interface is usually big and rather flat. In this review, we focused on the properties of protein- protein interactions, the interactions between these properties and the design of inhibitors. Computational methods predicting protein-protein interactions as well as classification and features of inhibitors targeting protein-protein interactions were also discussed. At last, an example of how to design inhibitors to block bindings of protein and protein was given.