生物活性 | |||
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描述 | The papain-like protease (PLpro) can process the viral polyprotein in a coordinated manner and strip ubiquitin and ISG15 from host-cell proteins to aid coronaviruses in their evasion of the host innate immune responses. Therefore, PLpro is an attractive antiviral drug target for its essential role for coronaviral replication[2]. PLpro inhibitor is a potent inhibitor against the PLpro from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have an IC50 value of 2.6 ± 0.1 μM. PLpro inhibitor displayed significant antiviral activity with an EC50 value of 13.1 ± 0.7 uM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlated with the in vitro inhibition of PLpro, suggesting that the compound works directly on the enzyme in cellshttp://www.google.com/patents/WO2010022355A1cl=en. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.89mL 0.58mL 0.29mL |
14.43mL 2.89mL 1.44mL |
28.87mL 5.77mL 2.89mL |
参考文献 |
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