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