临床批准的 MEK 抑制剂曲美替尼可有效阻断甲型流感病毒的传播和细胞因子表达。

The clinically approved MEK inhibitor Trametinib efficiently blocks influenza A virus propagation and cytokine expression.

机构信息

Institute of Virology (IVM), Westfälische Wilhelms-Universität, Münster, Germany; Cluster of Excellence "Cells in Motion", Westfälische Wilhelms-Universität, Münster, Germany.

Institute of Virology (IVM), Westfälische Wilhelms-Universität, Münster, Germany.

出版信息

Antiviral Res. 2018 Sep;157:80-92. doi: 10.1016/j.antiviral.2018.07.006. Epub 2018 Jul 7.

Abstract

Influenza A virus (IAV) infections are still a major global threat for humans, especially for the risk groups of young children and the elderly. Annual epidemics and sporadically occurring pandemics highlight the necessity of effective antivirals that can limit viral replication. The currently licensed antiviral drugs target viral factors and are prone to provoke viral resistance. In infected host cells IAV induces various cellular signaling cascades. The Raf/MEK/ERK signaling cascade is indispensable for IAV replication because it triggers the nuclear export of newly assembled viral ribonucleoproteins (vRNPs). Inhibition of this cascade limits viral replication. Thus, next to their potential in anti-tumor therapy, inhibitors targeting the Raf/MEK/ERK signaling cascade came into focus as potential antiviral drugs. The first licensed MEK inhibitor Trametinib (GSK-1120212) is used for treatment of malignant melanoma, being highly selective and having a promising side effect profile. Since Trametinib may be qualified for a repurposing approach that would significantly shorten development time for an anti-flu use, we evaluated its antiviral potency and mode of action. In this study, we describe that Trametinib efficiently blocks replication of different IAV subtypes in vitro and in vivo. The broad antiviral activity against various IAV strains was due to its ability to interfere with export of progeny vRNPs from the nucleus. The compound also limited hyper-expression of several cytokines. Thus, we show for the first time that a clinically approved MEK inhibitor acts as a potent anti-influenza agent.

摘要

甲型流感病毒(IAV)感染仍然是人类的主要全球威胁,尤其是对幼儿和老年人这两个风险群体。年度流行和偶发的大流行突出表明,需要有效的抗病毒药物来限制病毒复制。目前获得许可的抗病毒药物针对病毒因素,容易引发病毒耐药性。在感染宿主细胞中,IAV 诱导多种细胞信号级联反应。Raf/MEK/ERK 信号级联反应对于 IAV 复制是必不可少的,因为它触发了新组装的病毒核糖核蛋白(vRNP)的核输出。抑制该级联反应限制了病毒的复制。因此,除了在抗肿瘤治疗中的潜在作用外,靶向 Raf/MEK/ERK 信号级联的抑制剂作为潜在的抗病毒药物也引起了关注。第一个获得许可的 MEK 抑制剂 Trametinib(GSK-1120212)用于治疗恶性黑色素瘤,具有高度选择性和有前途的副作用谱。由于 Trametinib 可能有资格进行重新利用的方法,这将大大缩短抗流感药物的开发时间,我们评估了它的抗病毒效力和作用机制。在这项研究中,我们描述了 Trametinib 能够有效地在体外和体内阻断不同 IAV 亚型的复制。该化合物对各种 IAV 株的广泛抗病毒活性是由于其干扰核内新生 vRNP 输出的能力。该化合物还限制了几种细胞因子的过度表达。因此,我们首次表明,一种临床批准的 MEK 抑制剂作为一种有效的抗流感药物。

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