Suppr超能文献

BX795 的一种脱靶效应可阻断单纯疱疹病毒 1 型对眼部的感染。

An off-target effect of BX795 blocks herpes simplex virus type 1 infection of the eye.

机构信息

Department of Ophthalmology and Visual Sciences, University of Illinois Medical Center, Chicago, IL 60612, USA.

Department of Bioengineering, University of Illinois, Chicago, IL 60607, USA.

出版信息

Sci Transl Med. 2018 Feb 14;10(428). doi: 10.1126/scitranslmed.aan5861.

Abstract

Herpes simplex virus type 1 (HSV-1) causes recurrent mucocutaneous lesions in the eye that may advance to corneal blindness. Nucleoside analogs exemplified by acyclovir (ACV) form the primary class of antiherpetic drugs, but this class suffers limitations due to the emergence of viral resistance and other side effects. While studying the molecular basis of ocular HSV-1 infection, we observed that BX795, a commonly used inhibitor of TANK-binding kinase 1 (TBK1), strongly suppressed infection by multiple strains of HSV-1 in transformed and primary human cells, cultured human and animal corneas, and a murine model of ocular infection. Our investigations revealed that the antiviral activity of BX795 relies on targeting Akt phosphorylation in infected cells, leading to the blockage of viral protein synthesis. This small-molecule inhibitor, which was also effective against an ACV-resistant HSV-1 strain, shows promise as an alternative to existing drugs and as an effective topical therapy for ocular herpes infection. Collectively, our results obtained using multiple infection models and virus strains establish BX795 as a promising lead compound for broad-spectrum antiviral applications in humans.

摘要

单纯疱疹病毒 1 型 (HSV-1) 可引起眼部复发性黏膜皮肤损伤,进而导致角膜失明。以阿昔洛韦 (ACV) 为代表的核苷类似物是抗疱疹病毒药物的主要类别,但由于病毒耐药性和其他副作用的出现,该类别存在局限性。在研究眼单纯疱疹病毒 1 型感染的分子基础时,我们观察到 BX795,一种常用于 TANK 结合激酶 1 (TBK1) 的抑制剂,可强烈抑制转化和原代人细胞、培养的人及动物角膜以及眼部感染的小鼠模型中多种 HSV-1 株的感染。我们的研究表明,BX795 的抗病毒活性依赖于感染细胞中 Akt 磷酸化的靶向作用,从而阻断病毒蛋白的合成。这种小分子抑制剂对 ACV 耐药的 HSV-1 株也有效,有望成为现有药物的替代品,并作为眼部单纯疱疹感染的有效局部治疗药物。综上所述,我们使用多种感染模型和病毒株获得的结果表明,BX795 是一种有前途的广谱抗病毒应用的先导化合物。

相似文献

引用本文的文献

本文引用的文献

2
Acute kidney injury due to acyclovir.阿昔洛韦所致急性肾损伤
CEN Case Rep. 2013 May;2(1):38-40. doi: 10.1007/s13730-012-0035-0. Epub 2012 Oct 1.

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验