靶向蛋白非催化功能的药物开发新策略  

Targeting the Non-catalytic Functions of Proteins for New Drug Discovery

作　　者：杨欣语 宋宜辉 余斌[1] YANG Xinyu;SONG Yihui;YU Bin(Zhengzhou University School of Pharmaceutical Sciences,Zhengzhou 450001,China)

机构地区：[1]郑州大学药学院,河南郑州450001

出　　处：《药学进展》2022年第1期4-18,共15页Progress in Pharmaceutical Sciences

基　　金：国家自然科学基金(No.31900875,No.81973177)。

摘　　要：靶向蛋白催化功能的小分子抑制剂具有特异性差和临床副作用多等缺点,靶向蛋白的非催化功能在药物开发中具有较大的潜力。鉴于靶向蛋白非催化功能抑制剂的广阔的应用前景,对靶向蛋白非催化功能的抑制剂开发新策略即非催化功能结构域策略、变构调控策略和蛋白-蛋白相互作用策略进行总结,同时对其存在的问题和应用前景进行展望,以期为靶向蛋白非催化功能的药物开发提供方向。The small molecule inhibitors targeting the conserved catalytic function of proteins face such challenges as poor specificity and numerous side-effects, while targeting the non-catalytic functions of proteins has great potential for the development of drugs. In view of the wide prospects of inhibitors targeting the non-catalytic functions of proteins, this review briefly summarizes the new drug discovery strategies in this field, including non-catalytic functional domain strategy and the strategies of allosteric regulation and protein-protein interaction, with a prospect of their existing problems and future application, aiming to provide new directions for the development of drugs targeting the non-catalytic functions of proteins.

关 键 词：药物开发策略 蛋白非催化功能 变构调控 蛋白-蛋白相互作用 

分 类 号：R914[医药卫生—药物化学]