An overview of potential inhibitors targeting non-structural proteins 3 (PLpro and Mac1) and 5 (3CLpro/Mpro) of SARS-CoV-2,Computational and Structural Biotechnology Journal

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An overview of potential inhibitors targeting non-structural proteins 3 (PLpro and Mac1) and 5 (3CLpro/Mpro) of SARS-CoV-2
Computational and Structural Biotechnology Journal ( IF 4.4 ) Pub Date : 2021-08-24 , DOI: 10.1016/j.csbj.2021.08.036
Fangfang Yan ₁ , Feng Gao _{1,

2,

3}

Affiliation

There is an urgent need to develop effective treatments for coronavirus disease 2019 (COVID-19), which is caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). The rapid spread of SARS-CoV-2 has resulted in a global pandemic that has not only affected the daily lives of individuals but also had a significant impact on the global economy and public health. Although extensive research has been conducted to identify inhibitors targeting SARS-CoV-2, there are still no effective treatment strategies to combat COVID-19. SARS-CoV-2 comprises two important proteolytic enzymes, namely, the papain-like proteinase, located within non-structural protein 3 (nsp3), and nsp5, both of which cleave large replicase polypeptides into multiple fragments that are required for viral replication. Moreover, a domain within nsp3, known as the macrodomain (Mac1), also plays an important role in viral replication. Inhibition of their functions should be able to significantly interfere with the replication cycle of the virus, and therefore these key proteins may serve as potential therapeutic targets. The functions of the above viral targets and their corresponding inhibitors have been summarized in the current review. This review provides comprehensive updates of nsp3 and nsp5 inhibitor development and would help advance the discovery of novel anti-viral therapeutics against SARS-CoV-2.

中文翻译：

针对 SARS-CoV-2 非结构蛋白 3（PLpro 和 Mac1）和 5（3CLpro/Mpro）的潜在抑制剂概述

迫切需要开发针对 2019 年冠状病毒病 (COVID-19) 的有效治疗方法，该疾病是由严重急性呼吸综合征冠状病毒 2 (SARS-CoV-2) 引起的。 SARS-CoV-2的迅速传播已导致全球大流行，不仅影响了个人的日常生活，而且对全球经济和公共卫生产生了重大影响。尽管已经进行了大量研究来确定针对 SARS-CoV-2 的抑制剂，但仍然没有有效的治疗策略来对抗 COVID-19。 SARS-CoV-2 包含两种重要的蛋白水解酶，即位于非结构蛋白 3 (nsp3) 内的木瓜蛋白酶和 nsp5，这两种酶均可将大的复制酶多肽切割成病毒复制所需的多个片段。此外，nsp3 内的一个结构域，称为宏结构域 (Mac1)，在病毒复制中也发挥着重要作用。抑制它们的功能应该能够显着干扰病毒的复制周期，因此这些关键蛋白可能作为潜在的治疗靶点。本综述对上述病毒靶点及其相应抑制剂的功能进行了总结。这篇综述提供了 nsp3 和 nsp5 抑制剂开发的全面更新，将有助于推进针对 SARS-CoV-2 的新型抗病毒疗法的发现。

更新日期：2021-08-24

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