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PIKfyve 特异性抑制剂在体外限制多种冠状病毒的复制,但不能在 COVID-19 的小鼠模型中复制。

PIKfyve-specific inhibitors restrict replication of multiple coronaviruses in vitro but not in a murine model of COVID-19.

机构信息

Department of Microbiology and Immunology, University of Maryland, School of Medicine, 685 West Baltimore St, Baltimore, MD, 21201, USA.

Center for Pathogen Research, University of Maryland, School of Medicine, 685 West Baltimore St, Baltimore, MD, 21201, USA.

出版信息

Commun Biol. 2022 Aug 12;5(1):808. doi: 10.1038/s42003-022-03766-2.

Abstract

The ongoing COVID-19 pandemic has claimed more than 6 million lives and continues to test the world economy and healthcare systems. To combat this pandemic, the biological research community has shifted efforts to the development of medical countermeasures, including vaccines and therapeutics. However, to date, the only small molecules approved for the treatment of COVID-19 in the United States are the nucleoside analogue Remdesivir and the protease inhibitor Paxlovid, though multiple compounds have received Emergency Use Authorization and many more are currently being tested in human efficacy trials. One such compound, Apilimod, is being considered as a COVID-19 therapeutic in a Phase II efficacy trial. However, at the time of writing, there are no published efficacy data in human trials or animal COVID-19 models. Here we show that, while Apilimod and other PIKfyve inhibitors have potent antiviral activity in various cell lines against multiple human coronaviruses, these compounds worsen disease in a COVID-19 murine model when given prophylactically or therapeutically.

摘要

持续的 COVID-19 大流行已导致超过 600 万人死亡,并继续考验着世界经济和医疗体系。为了应对这一大流行病,生物研究界已将努力转向医疗对策的开发,包括疫苗和疗法。然而,迄今为止,在美国获得批准用于治疗 COVID-19 的唯一小分子药物是核苷类似物瑞德西韦和蛋白酶抑制剂帕罗韦德,尽管有多种化合物已获得紧急使用授权,还有许多正在进行人体疗效试验。阿匹莫德就是一种在 II 期疗效试验中被考虑用于治疗 COVID-19 的化合物。然而,在撰写本文时,尚无在人体试验或动物 COVID-19 模型中发表的疗效数据。在这里,我们表明,虽然阿匹莫德和其他 PIKfyve 抑制剂在多种细胞系中对多种人类冠状病毒具有强大的抗病毒活性,但这些化合物在预防性或治疗性给药时会使 COVID-19 小鼠模型的疾病恶化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4864/9374771/1af8f5342619/42003_2022_3766_Fig1_HTML.jpg

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