小分子抗肿瘤共价药物的研究进展

Progress of small molecule anti-tumor covalent drugs

共价药物是一类能与靶标形成共价键从而发挥生物学功能的药物。随着多个激酶抑制剂类抗肿瘤共价药物的上市,共价药物重新回到药物发现的视野并成为抗肿瘤化疗药物的研究热点。本文从共价药物的作用机制、药理学优势、开发策略以及近年来出现的抗肿瘤共价药物及候选药物的研究进展进行综述,为新型抗肿瘤共价药物的设计提供参考。

Covalent drugs are a type of inhibitors which exert their biological functions by irreversibly binding to the target through covalent bonds.With the marketing of kinase inhibitor covalent drugs against tumor,covalent drugs have regained the attention for drug discovery and have become a recent hotspot of anti-tumor drugs.In this paper,the action mechanisms,pharmacological advantages and the development strategies of modern covalent drugs are discussed and the recent research progress of anti-tumor covalent inhibitors is summarized,which provides a reference for the design of new anti-tumor covalent drugs.