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摘要
严重的急性呼吸系统综合症冠状病毒2(SARS-CoV-2)已在世界范围内传播,并造成了广泛的破坏。在没有明确治疗的情况下,对症治疗仍然是护理的标准。正在尝试重新利用许多现有药物,包括几种抗病毒药物,以解决COVID-19大流行。但是,大多数都未能在临床试验中显示出明显的益处。一种有吸引力的方法可能是靶向与SARS-CoV-2发病机理有关的宿主蛋白酶。通过跨膜丝氨酸蛋白酶2(TMPRSS2)的蛋白水解切割来引发病毒的刺突(S)蛋白,对于病毒与宿主细胞结合到其受体血管紧张素转化酶2(ACE2)后的融合,对于病毒与宿主细胞的融合是必需的。 )。还有其他具有不同时空位置的蛋白酶,可能对病毒进入和随后在细胞内复制很重要,这些蛋白酶包括胰蛋白酶,弗林蛋白酶和组织蛋白酶。在本报告中,我们讨论了TMPRSS2抑制剂,组织蛋白酶,胰蛋白酶,弗林蛋白酶,纤溶酶,X因子和弹性蛋白酶在由SARS-CoV-2引起的感染中的初步治疗作用。讨论了可用的证据和假设,重点讨论了已被批准用于其他适应症的药物,例如溴己定,氯化铵,萘法莫司,卡莫司他,氨甲环酸,ε-氨基己酸,氯喹,乌司他丁,抑肽酶和抗凝药。同时,还讨论了正在测试的新型化合物以及使用这些试剂的问题。
关键词: COVID-19,TMPRSS,组织蛋白酶,弗林蛋白酶,纤溶酶,氯喹。
Current Drug Targets
Title:Targeting Host Cell Proteases to Prevent SARS-CoV-2 Invasion
Volume: 22 Issue: 2
关键词: COVID-19,TMPRSS,组织蛋白酶,弗林蛋白酶,纤溶酶,氯喹。
摘要: Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) has spread worldwide and caused widespread devastation. In the absence of definitive therapy, symptomatic management remains the standard of care. Repurposing of many existing drugs, including several anti-viral drugs, is being attempted to tackle the COVID-19 pandemic. However, most of them have failed to show significant benefit in clinical trials. An attractive approach may be to target host proteases involved in SARS-CoV-2 pathogenesis. The priming of the spike (S) protein of the virus by proteolytic cleavage by the transmembrane serine protease-2 (TMPRSS2) is necessary for the fusion of the virus to the host cell after it binds to its receptor angiotensin converting enzyme-2 (ACE2). There are other proteases with varying spatiotemporal locations that may be important for viral entry and subsequent replication inside the cells, and these include trypsin, furin and cathepsins. In this report, we have discussed the tentative therapeutic role of inhibitors of TMPRSS2, cathepsin, trypsin, furin, plasmin, factor X and elastase in infection caused by SARS-CoV-2. Both available evidence, as well as hypotheses, are discussed, with emphasis on drugs which are approved for other indications such as bromhexine, ammonium chloride, nafamostat, camostat, tranexamic acid, epsilon amino-caproic acid, chloroquine, ulinastatin, aprotinin and anticoagulant drugs. Simultaneously, novel compounds being tested and problems with using these agents are also discussed.
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Cite this article as:
Targeting Host Cell Proteases to Prevent SARS-CoV-2 Invasion, Current Drug Targets 2021; 22 (2) . https://dx.doi.org/10.2174/1389450121666200924113243
DOI https://dx.doi.org/10.2174/1389450121666200924113243 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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