Department of Experimental, Diagnostic and Specialty Medicine, University of Bologna, 40138 Bologna, Italy.
Department of Biomedical and Clinical Sciences (BKV), Linköping University, SE-58183 Linköping, Sweden.
Int J Mol Sci. 2020 May 15;21(10):3492. doi: 10.3390/ijms21103492.
Following the outbreak of novel severe acute respiratory syndrome (SARS)-coronavirus (CoV)2, the majority of nations are struggling with countermeasures to fight infection, prevent spread and improve patient survival. Considering that the pandemic is a recent event, no large clinical trials have been possible and since coronavirus specific drug are not yet available, there is no strong consensus on how to treat the coronavirus disease 2019 (COVID-19) associated viral pneumonia. Coronaviruses code for an important multifunctional enzyme named papain-like protease (PLP), that has many roles in pathogenesis. First, PLP is one of the two viral cysteine proteases, along with 3-chymotripsin-like protease, that is responsible for the production of the replicase proteins required for viral replication. Second, its intrinsic deubiquitinating and deISGylating activities serve to antagonize the host's immune response that would otherwise hinder infection. Both deubiquitinating and deISGylating functions involve the removal of the small regulatory polypeptides, ubiquitin and ISG15, respectively, from target proteins. Ubiquitin modifications can regulate the innate immune response by affecting regulatory proteins, either by altering their stability via the ubiquitin proteasome pathway or by directly regulating their activity. ISG15 is a ubiquitin-like modifier with pleiotropic effects, typically expressed during the host cell immune response. PLP inhibitors have been evaluated during past coronavirus epidemics, and have showed promising results as an antiviral therapy in vitro. In this review, we recapitulate the roles of PLPs in coronavirus infections, report a list of PLP inhibitors and suggest possible therapeutic strategies for COVID-19 treatment, using both clinical and preclinical drugs.
新型严重急性呼吸综合征冠状病毒(SARS-CoV-2)爆发后,大多数国家都在努力采取对策来对抗感染、阻止传播和提高患者生存率。鉴于此次大流行是最近发生的事件,因此不可能进行大规模临床试验,而且由于尚未开发出针对冠状病毒的特定药物,因此对于如何治疗 2019 年冠状病毒病(COVID-19)相关病毒性肺炎尚未达成共识。冠状病毒编码一种名为木瓜样蛋白酶(PLP)的重要多功能酶,该酶在发病机制中具有多种作用。首先,PLP 是两种病毒半胱氨酸蛋白酶之一,与 3-糜蛋白酶样蛋白酶一起,负责产生病毒复制所需的复制酶蛋白。其次,其内在的去泛素化和去 ISG 化活性可拮抗宿主的免疫反应,否则该免疫反应会阻碍感染。去泛素化和去 ISG 化功能均涉及从小调节多肽(分别为泛素和 ISG15)上去除靶蛋白。泛素修饰可通过影响调节蛋白来调节先天免疫反应,或者通过泛素蛋白酶体途径改变其稳定性,或者直接调节其活性。ISG15 是一种具有多种作用的泛素样修饰物,通常在宿主细胞免疫反应期间表达。过去在冠状病毒流行期间已经评估了 PLP 抑制剂,并在体外作为抗病毒疗法显示出有希望的结果。在这篇综述中,我们回顾了 PLP 在冠状病毒感染中的作用,报告了 PLP 抑制剂的列表,并提出了使用临床和临床前药物治疗 COVID-19 的可能治疗策略。