Repurposing and discovery of transmembrane serine protease 2 (TMPRSS2) inhibitors as prophylactic therapies for new coronavirus disease 2019 (COVID-19).

IF 1.5 4区 医学 Q4 CHEMISTRY, MEDICINAL Pharmazie Pub Date : 2023-12-04 DOI:10.1691/ph.2023.3578
Hao Yang, Xinxin Lin, Qimeng Yu, Annoor Awadasseid, Wen Zhang
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Abstract

The global pandemic of COVID-19 disease is caused by the pathogenic factor called SARS-CoV-2. Meanwhile, a series of vaccines and small-molecule drugs, including the mRNA vaccines and Paxlovid®, have been approved, but their efficacy is decreased significantly due to the constant emergence of mutant viral strains. The R&D of host-directed therapeutics has great potential to overcome such limitations and provide new prevention and therapy options for patients with COVID-19 or high-risk group for SARS-CoV-2 infections. Transmembrane serine protease 2 (TMPRSS2) is belonging to a protein family with highly conserved serine protease domain whose crucial role in viral entry is to activate the spike protein of viruses to induce the fusion between host cells and viruses. In this review, we sketch the critical position of TMPRSS2 in the SARS-CoV-2 viral entry and summarize the advanced research and development of TMPRSS2 inhibitors, including repurposed drugs, as a new way to fight COVID-19.

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将跨膜丝氨酸蛋白酶 2 (TMPRSS2) 抑制剂作为 2019 年新型冠状病毒疾病的预防性疗法的再利用和发现(COVID-19)。
全球大流行的 COVID-19 疾病是由名为 SARS-CoV-2 的致病因子引起的。与此同时,包括 mRNA 疫苗和 Paxlovid® 在内的一系列疫苗和小分子药物已获得批准,但由于变异病毒株的不断出现,其疗效明显降低。宿主导向疗法的研发具有巨大潜力,可以克服这些局限性,为 COVID-19 患者或 SARS-CoV-2 感染的高危人群提供新的预防和治疗方案。跨膜丝氨酸蛋白酶 2(TMPRSS2)属于蛋白家族,具有高度保守的丝氨酸蛋白酶结构域,其在病毒进入过程中的关键作用是激活病毒的尖峰蛋白,诱导宿主细胞与病毒融合。在这篇综述中,我们概述了TMPRSS2在SARS-CoV-2病毒进入过程中的关键地位,并总结了TMPRSS2抑制剂(包括再利用药物)作为抗击COVID-19新途径的先进研究和开发。
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来源期刊
Pharmazie
Pharmazie 医学-化学综合
CiteScore
3.10
自引率
0.00%
发文量
56
审稿时长
1.2 months
期刊介绍: The journal DiePharmazie publishs reviews, experimental studies, letters to the editor, as well as book reviews. The following fields of pharmacy are covered: Pharmaceutical and medicinal chemistry; Pharmaceutical analysis and drug control; Pharmaceutical technolgy; Biopharmacy (biopharmaceutics, pharmacokinetics, biotransformation); Experimental and clinical pharmacology; Pharmaceutical biology (pharmacognosy); Clinical pharmacy; History of pharmacy.
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