Drug Repurposing for the SARS-CoV-2 Papain-Like Protease,ChemMedChem

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Drug Repurposing for the SARS-CoV-2 Papain-Like Protease
ChemMedChem ( IF 3.6 ) Pub Date : 2021-08-22 , DOI: 10.1002/cmdc.202100455
Chia-Chuan Cho ₁ , Shuhua G Li ₁ , Tyler J Lalonde ₁ , Kai S Yang ₁ , Ge Yu ₁ , Yuchen Qiao ₁ , Shiqing Xu ₁ , Wenshe Ray Liu _{1,

2,

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Affiliation

Papain-like protease (PLpro) is a cysteine protease with deubiquitination and deISGylation activities, and is essential for SARS-CoV-2 replication and pathogenesis. By screening 33 deubiquitinase inhibitors and 37 cysteine protease inhibitors, we discovered that a number of molecules are potent PLpro inhibitors such as TCID, PR-619, and SJB2-043. Among these inhibitors, SJB2-043 has an outstanding IC₅₀ value of 0.56 μM, but only shows partial inhibition of papain-like protease. It binds likely to an allosteric site of PLpro to convene its inhibition effect.

中文翻译：

SARS-CoV-2 类木瓜蛋白酶的药物再利用

木瓜蛋白酶样蛋白酶(PLpro) 是一种半胱氨酸蛋白酶，具有去泛素化和去糖基化活性，对于 SARS-CoV-2 复制和发病机制至关重要。通过筛选33种去泛素酶抑制剂和37种半胱氨酸蛋白酶抑制剂，我们发现许多分子是有效的PLpro抑制剂，例如TCID、PR-619和SJB2-043。在这些抑制剂中，SJB2-043具有0.56 μM的出色IC ₅₀值，但仅表现出对木瓜蛋白酶样蛋白酶的部分抑制。它可能与 PLpro 的变构位点结合以发挥其抑制作用。

更新日期：2021-08-22

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