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揭示流感非结构蛋白 1 中可成药的新结合口袋:作为流感抗病毒靶点的 NS1-宿主相互作用。

Unveiling New Druggable Pockets in Influenza Non-Structural Protein 1: NS1-Host Interactions as Antiviral Targets for Flu.

机构信息

Coimbra Chemistry Center-Institute of Molecular Sciences (CQC-IMS), Department of Chemistry, University of Coimbra, 3004-535 Coimbra, Portugal.

BSIM Therapeutics, Instituto Pedro Nunes, 3030-199 Coimbra, Portugal.

出版信息

Int J Mol Sci. 2023 Feb 3;24(3):2977. doi: 10.3390/ijms24032977.

Abstract

Influenza viruses are responsible for significant morbidity and mortality worldwide in winter seasonal outbreaks and in flu pandemics. Influenza viruses have a high rate of evolution, requiring annual vaccine updates and severely diminishing the effectiveness of the available antivirals. Identifying novel viral targets and developing new effective antivirals is an urgent need. One of the most promising new targets for influenza antiviral therapy is non-structural protein 1 (NS1), a highly conserved protein exclusively expressed in virus-infected cells that mediates essential functions in virus replication and pathogenesis. Interaction of NS1 with the host proteins PI3K and TRIM25 is paramount for NS1's role in infection and pathogenesis by promoting viral replication through the inhibition of apoptosis and suppressing interferon production, respectively. We, therefore, conducted an analysis of the druggability of this viral protein by performing molecular dynamics simulations on full-length NS1 coupled with ligand pocket detection. We identified several druggable pockets that are partially conserved throughout most of the simulation time. Moreover, we found out that some of these druggable pockets co-localize with the most stable binding regions of the protein-protein interaction (PPI) sites of NS1 with PI3K and TRIM25, which suggests that these NS1 druggable pockets are promising new targets for antiviral development.

摘要

流感病毒在冬季季节性爆发和流感大流行期间在全球范围内导致了很高的发病率和死亡率。流感病毒具有很高的进化率,需要每年更新疫苗,这严重降低了现有抗病毒药物的效果。寻找新的病毒靶点和开发新的有效抗病毒药物是当务之急。流感抗病毒治疗最有前途的新靶点之一是非结构蛋白 1(NS1),这是一种高度保守的蛋白,仅在病毒感染的细胞中表达,介导病毒复制和发病机制中的基本功能。NS1 与宿主蛋白 PI3K 和 TRIM25 的相互作用对于 NS1 在感染和发病机制中的作用至关重要,它通过抑制细胞凋亡促进病毒复制,并抑制干扰素的产生。因此,我们通过对全长 NS1 进行分子动力学模拟并结合配体口袋检测,对该病毒蛋白的可药性进行了分析。我们确定了几个具有部分保守性的可成药性口袋,这些口袋在整个模拟过程中的大部分时间内都存在。此外,我们发现其中一些可成药性口袋与 NS1 与 PI3K 和 TRIM25 的蛋白-蛋白相互作用(PPI)结合区域的最稳定结合区域重合,这表明这些 NS1 可成药性口袋是开发抗病毒药物的有前途的新靶点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3b9c/9918223/54d77f00ae43/ijms-24-02977-g001.jpg

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