Inhibition of SARS-CoV-2 Entry into Host Cells Using Small Molecules.
Inhibition of SARS-CoV-2 Entry into Host Cells Using Small Molecules.
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DOI：
10.3390/ph13120447
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发表时间：
2020-12-08
期刊：
影响因子：
--
通讯作者：
Lee S
中科院分区：
文献类型：
--
作者：
Al Adem K;Shanti A;Stefanini C;Lee S
严重急性呼吸系统综合症冠状病毒 2 (SARS-CoV-2) 是一种属于冠状病毒家族的病毒，目前已知会引起冠状病毒病 (Covid-19)，该疾病于 2019 年 12 月首次被发现。Covid-19 会导致从轻度感染到肺炎和肺衰竭等呼吸道疾病。引人注目的是，在首次报告后的几个月内，Covid-19 以异常高的速度在全球传播，并造成了巨大的人员伤亡。到目前为止，还没有针对 Covid-19 的具体治疗方法。设计能够干扰病毒进入过程的抑制药物是早期对抗 SARS-CoV-2 感染的主要预防疗法之一。在这篇综述中，我们简要介绍了冠状病毒的主要特征，讨论了SARS-CoV-2进入人类宿主细胞的机制，并综述了抑制SARS-CoV-2进入宿主细胞的小分子。具体来说，我们专注于通过实验验证和/或计算预测确定的小分子，这些小分子以 SARS-CoV-2 刺突蛋白、人血管紧张素转换酶 2 (ACE2) 受体和激活病毒融合的不同宿主细胞蛋白酶为目标。鉴于迄今为止 Covid-19 病例持续增加，应努力验证这些已确定的小分子抑制剂的治疗效果。
Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), a virus belonging to the Coronavirus family, is now known to cause Coronavirus Disease (Covid-19) which was first recognized in December 2019. Covid-19 leads to respiratory illnesses ranging from mild infections to pneumonia and lung failure. Strikingly, within a few months of its first report, Covid-19 has spread worldwide at an exceptionally high speed and it has caused enormous human casualties. As yet, there is no specific treatment for Covid-19. Designing inhibitory drugs that can interfere with the viral entry process constitutes one of the main preventative therapies that could combat SARS-CoV-2 infection at an early stage. In this review, we provide a brief introduction of the main features of coronaviruses, discuss the entering mechanism of SARS-CoV-2 into human host cells and review small molecules that inhibit SARS-CoV-2 entry into host cells. Specifically, we focus on small molecules, identified by experimental validation and/or computational prediction, that target the SARS-CoV-2 spike protein, human angiotensin converting enzyme 2 (ACE2) receptor and the different host cell proteases that activate viral fusion. Given the persistent rise in Covid-19 cases to date, efforts should be directed towards validating the therapeutic effectiveness of these identified small molecule inhibitors.
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