A collection of twelve organoselenium compounds, structural analogues of antioxidant drug ebselen were screened for inhibition of the papain-like protease (PL^pro) from the acute respiratory syndrome coronavirus 2 (SARS-CoV-2, CoV2). This cysteine protease, being responsible for the hydrolysis of peptide bonds between specific amino acids, plays a critical role in CoV2 replication and in assembly of new viral particles within human cells. The activity of the PL^pro CoV2 is essential for the progression of coronavirus disease 2019 (COVID-19) and it constitutes a key target for the development of anti-COVID-19 drugs. Here, we identified four strong inhibitors that bind favorably to the PL^pro CoV2 with the IC₅₀ in the nanomolar range.

中文翻译：

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通过筛选含硒化合物的文库发现PLproCoV2的有效抑制剂

筛选了十二种有机硒化合物（抗氧化剂药物ebselen的结构类似物）以抑制来自急性呼吸系统综合症冠状病毒2（SARS-CoV-2，CoV2）的木瓜蛋白酶（PL ^pro）。这种半胱氨酸蛋白酶负责水解特定氨基酸之间的肽键，在CoV2复制和人类细胞内新病毒颗粒的组装中起关键作用。PL ^pro CoV2的活性对于2019年冠状病毒疾病（COVID-19）的发展至关重要，它构成了抗COVID-19药物开发的关键目标。在这里，我们确定了四种强抑制剂，它们以纳摩尔范围的IC ₅₀与PL ^pro CoV2良好结合。