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针对 furin,一种细胞蛋白前体转化酶,用于 COVID-19 的预防和治疗。

Targeting furin, a cellular proprotein convertase, for COVID-19 prevention and therapeutics.

机构信息

Key Laboratory of Epigenetics and Oncology, The Research Center for Preclinical Medicine, Southwest Medical University, Luzhou, China; Department of Reproductive Medicine, The Affiliated Hospital, Southwest Medical University, Luzhou, Sichuan, China; The State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Macau.

Key Laboratory of Epigenetics and Oncology, The Research Center for Preclinical Medicine, Southwest Medical University, Luzhou, China; School of Basic Medicine, Southwest Medical University, Luzhou, Sichuan, China.

出版信息

Drug Discov Today. 2024 Jul;29(7):104026. doi: 10.1016/j.drudis.2024.104026. Epub 2024 May 17.

Abstract

SARS-CoV-2 has triggered an international outbreak of the highly contagious acute respiratory disease known as COVID-19. Identifying key targets in the virus infection lifecycle is crucial for developing effective prevention and therapeutic strategies against it. Furin is a serine endoprotease that belongs to the family of proprotein convertases and plays a critical role in the entry of host cells by SARS-CoV-2. Furin can cleave a specific S1/S2 site, PRRAR, on the spike protein of SARS-CoV-2, which promotes viral transmission by facilitating membrane fusion. Hence, targeting furin could hold clinical implications for the prevention and treatment of COVID-19. This review offers an overview of furin's structure, substrates, function, and inhibitors, with a focus on its potential role in SARS-CoV-2 infection.

摘要

SARS-CoV-2 引发了一种高度传染性的急性呼吸道疾病的国际爆发,这种疾病被称为 COVID-19。确定病毒感染生命周期中的关键靶标对于开发针对它的有效预防和治疗策略至关重要。弗林是一种丝氨酸内肽酶,属于蛋白原转化酶家族,在 SARS-CoV-2 进入宿主细胞中发挥关键作用。弗林可以切割 SARS-CoV-2 刺突蛋白上的特定 S1/S2 位点 PRRAR,通过促进膜融合促进病毒传播。因此,靶向弗林可能对 COVID-19 的预防和治疗具有临床意义。本综述概述了弗林的结构、底物、功能和抑制剂,重点介绍了其在 SARS-CoV-2 感染中的潜在作用。

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