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用于药物再利用的 SARS-CoV-2 主要蛋白酶抑制剂的系统搜索:依他尼酸作为一种潜在药物。

Systematic Search for SARS-CoV-2 Main Protease Inhibitors for Drug Repurposing: Ethacrynic Acid as a Potential Drug.

机构信息

Department of Basic Medical Sciences, Neurosciences and Sense Organs, University of Bari Aldo Moro, Piazza G. Cesare 11, 70124 Bari, Italy.

Department of Medicine, University Campus Bio-Medico of Rome, Via Alvaro del Portillo 21, 00128 Rome, Italy.

出版信息

Viruses. 2021 Jan 13;13(1):106. doi: 10.3390/v13010106.

Abstract

In 2019 an outbreak occurred which resulted in a global pandemic. The causative agent has been identified in a virus belonging to the family, similar to the agent of SARS, referred to as SARS-CoV-2. This epidemic spread rapidly globally with high morbidity and mortality. Although vaccine development is at a very advanced stage, there are currently no truly effective antiviral drugs to treat SARS-CoV-2 infection. In this study we present systematic and integrative antiviral drug repurposing effort aimed at identifying, among the drugs already authorized for clinical use, some active inhibitors of the SARS-CoV-2 main protease. The most important result of this analysis is the demonstration that ethacrynic acid, a powerful diuretic, is revealed to be an effective inhibitor of SARS-CoV-2 main protease. Even with all the necessary cautions, given the particular nature of this drug, these data can be the starting point for the development of an effective therapeutic strategy against SARS-CoV-2.

摘要

2019 年暴发了一次疫情,导致全球大流行。病原体已被确定为一种属于冠状病毒科的病毒,类似于 SARS 病原体,称为 SARS-CoV-2。这种流行病在全球迅速传播,发病率和死亡率都很高。尽管疫苗的开发已经处于非常先进的阶段,但目前还没有真正有效的抗病毒药物来治疗 SARS-CoV-2 感染。在这项研究中,我们进行了系统的和综合的抗病毒药物再利用努力,旨在从已经批准用于临床的药物中,确定一些可有效抑制 SARS-CoV-2 主要蛋白酶的药物。这项分析最重要的结果是表明,一种强有力的利尿剂依他尼酸被证明是 SARS-CoV-2 主要蛋白酶的有效抑制剂。尽管需要考虑到这种药物的特殊性质,但这些数据可以作为开发针对 SARS-CoV-2 的有效治疗策略的起点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/feea/7828626/f9903b701793/viruses-13-00106-g001.jpg

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