首页|靶向SARS-CoV-2 PLpro抑制剂的研究进展

靶向SARS-CoV-2 PLpro抑制剂的研究进展

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2019年末,新型冠状病毒(SARS-CoV-2),即严重急性呼吸系统综合征冠状病毒2席卷全球,对社会经济和人类健康造成了不可逆转的危害,相应的抗病毒药物研发也因此受到了广泛关注。SARS-CoV-2主要通过飞沫传播,并在宿主细胞内经历复制、转录与翻译过程后,以胞吞形式排出成熟病毒,构成感染闭环。值得注意的是,非结构蛋白3(nsp3)编码的木瓜蛋白酶样蛋白酶(PLpro)在这个过程中发挥着重要作用。同时在去泛素化等炎症反应中,PLpro也会帮助病毒逃避相应的免疫反应。因此,靶向抑制PLpro,不仅能够阻断病毒整体的复制过程,也可以恢复宿主自身的免疫功能,从而达到更好的抗SARS-CoV-2效果。综上,本文拟从化合物的不同结构出发,对近年来靶向SARS-CoV-2 PLpro的抑制剂研究进行探索性总结,以期为抗SARS-CoV-2的药物发现提供理论参考。
Research Progress in SARS-CoV-2 PLpro Inhibitors
Since the end of 2019,the new coronavirus swept the world,causing irreversible harm to social economy and human health,so the search for corresponding antiviral drugs has aroused wide attention.SARS-CoV-2 is mainly transmitted by droplets,and after the process of replication,transcription and translation in the host cell,the mature virus is excreted in the form of endocytosis,forming a closed loop of infection.Notably,the papain like protease(PLpro)encoded by non-structural protein 3(nsp3)plays an important role in this process.At the same time,PLpro also helps the virus evade the corresponding immune response in inflammatory reactions such as deubiquitination.Therefore,targeted inhibition of PLpro can not only block the overall replication process of the virus,but also restore the host's own immune function,so as to achieve a better anti-SARS-CoV-2 effect.In summary,based on the different structures of the compounds,this paper intends to conduct an exploratory summary of the recent studies on inhibitor targeting SARS-CoV-2 PLpro,in order to provide theoretical reference for the discovery of anti-SARS-CoV-2 drugs.

SARS-CoV-2PLpro targetinhibitortherapeutic drug

高雨、张国宁、王玉成

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中国医学科学院医药生物技术研究所,北京 100050

新型冠状病毒 木瓜蛋白酶样蛋白酶靶点 抑制剂 治疗药物

2024

中国药学杂志
中国药学会

中国药学杂志

CSTPCD北大核心
影响因子:0.957
ISSN:1001-2494
年,卷(期):2024.59(23)