TY - JOUR
T1 - An off-target effect of BX795 blocks herpes simplex virus type 1 infection of the eye
AU - Jaishankar, Dinesh
AU - Yakoub, Abraam M.
AU - Yadavalli, Tejabhiram
AU - Agelidis, Alex
AU - Thakkar, Neel
AU - Hadigal, Satvik
AU - Ames, Joshua
AU - Shukla, Deepak
N1 - Funding Information:
This work was supported by a grant from the National Eye Institute (R01 EY024710) to D.S.
Publisher Copyright:
Copyright © 2018 The Authors, some rights reserved.
PY - 2018/2/14
Y1 - 2018/2/14
N2 - 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.
AB - 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.
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U2 - 10.1126/scitranslmed.aan5861
DO - 10.1126/scitranslmed.aan5861
M3 - Article
C2 - 29444978
AN - SCOPUS:85042067967
SN - 1946-6234
VL - 10
JO - Science translational medicine
JF - Science translational medicine
IS - 428
M1 - aan5861
ER -