Back to Search Start Over

Anticancer pan-ErbB inhibitors reduce inflammation and tissue injury and exert broad-spectrum antiviral effects.

Authors :
Saul S
Karim M
Ghita L
Huang PT
Chiu W
Durán V
Lo CW
Kumar S
Bhalla N
Leyssen P
Alem F
Boghdeh NA
Tran DH
Cohen CA
Brown JA
Huie KE
Tindle C
Sibai M
Ye C
Khalil AM
Martinez-Sobrido L
Dye JM
Pinsky BA
Ghosh P
Das S
Solow-Cordero DE
Jin J
Wikswo JP
Jochmans D
Neyts J
Jonghe S
Narayanan A
Einav S
Source :
BioRxiv : the preprint server for biology [bioRxiv] 2023 May 10. Date of Electronic Publication: 2023 May 10.
Publication Year :
2023

Abstract

Targeting host factors exploited by multiple viruses could offer broad-spectrum solutions for pandemic preparedness. Seventeen candidates targeting diverse functions emerged in a screen of 4,413 compounds for SARS-CoV-2 inhibitors. We demonstrated that lapatinib and other approved inhibitors of the ErbB family receptor tyrosine kinases suppress replication of SARS-CoV-2, Venezuelan equine encephalitis virus (VEEV), and other emerging viruses with a high barrier to resistance. Lapatinib suppressed SARS-CoV-2 entry and later stages of the viral life cycle and showed synergistic effect with the direct-acting antiviral nirmatrelvir. We discovered that ErbB1, 2 and 4 bind SARS-CoV-2 S1 protein and regulate viral and ACE2 internalization, and they are required for VEEV infection. In human lung organoids, lapatinib protected from SARS-CoV-2-induced activation of ErbB-regulated pathways implicated in non-infectious lung injury, pro-inflammatory cytokine production, and epithelial barrier injury. Lapatinib suppressed VEEV replication, cytokine production and disruption of the blood-brain barrier integrity in microfluidic-based human neurovascular units, and reduced mortality in a lethal infection murine model. We validated lapatinib-mediated inhibition of ErbB activity as an important mechanism of antiviral action. These findings reveal regulation of viral replication, inflammation, and tissue injury via ErbBs and establish a proof-of-principle for a repurposed, ErbB-targeted approach to combat emerging viruses.

Details

Language :
English
Database :
MEDLINE
Journal :
BioRxiv : the preprint server for biology
Accession number :
34159337
Full Text :
https://doi.org/10.1101/2021.05.15.444128