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新型冠状病毒蛋白酶抑制剂研究进展

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由SARS-CoV-2引起的新型冠状病毒肺炎(COVID-19)已经造成数百万人死亡,至今仍未停止传播,给人类健康和社会稳定造成了严重的影响.SARS-CoV-2的蛋白酶包括PL蛋白酶和3CL蛋白酶,具有切割多聚蛋白和抑制宿主先天性免疫反应等功能,在冠状病毒的生命周期中起重要作用.PL蛋白酶和3CL蛋白酶在不同冠状病毒中基因序列高度保守,是开发抗冠状病毒药物的理想靶点.根据蛋白酶与抑制剂的结合方式不同,将已报道的抑制剂分为共价抑制剂和非共价抑制剂,分别介绍了 PL蛋白酶抑制剂和3CL蛋白酶的研究现状及不同抑制剂的作用特点、设计思路、化学结构及其生物活性,以期为抗冠状病毒药物的研发提供参考.
Progress Research on Inhibitors of SARS-CoV-2 Protease
The novel coronavirus pneumonia(CO VID-19)caused by SARS-CoV-2 has caused millions of deaths,and has not stopped spreading,which has caused serious impact on human health and social stability.The proteases of SARS-CoV-2 include PL protease and 3CL protease,which have functions on cleaving polyprotein and inhibiting host innate immune response,which play an important role in the life cycle of coronavirus.PL protease and 3CL protease have highly conserved gene sequences in different coronaviruses,making them ideal targets for developing anti coronavirus drugs.The author of this article divides the reported inhibitors into covalent inhibitors and noncovalent inhibitors based on the different binding modes of proteases and inhibitors.And introduce the research progress of PL protease and 3CL protease inhibitors,respectively,as well as the characteristics,design ideas,chemical structures,and biological activities of different inhibitors,in order to provide reference for the development of anti-coronavirus drugs.

coronavirusCOVID-19proteaseinhibitor

陈昕尧、张岩、蒋翔锐、杨鹏

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沈阳药科大学无涯创新学院,辽宁沈阳 110016

南通长三角药物高等研究院,江苏南通 226133

中科环渤海(烟台)药物高等研究院烟台新药创制山东省实验室,山东烟台 264117

中国科学院上海药物研究所,上海 201203

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冠状病毒 COVID-19 蛋白酶 抑制剂

2024

山东化工
山东省化工研究院 山东省化工信息中心

山东化工

影响因子:0.249
ISSN:1008-021X
年,卷(期):2024.53(15)