首页|Pharmacologic profiling reveals lapatinib as a novel antiviral against SARS-CoV-2 in vitro
Pharmacologic profiling reveals lapatinib as a novel antiviral against SARS-CoV-2 in vitro
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NSTL
Elsevier
The emergence of SARS-CoV-2 virus has resulted in a worldwide pandemic, but effective antiviral therapies are not widely available. To improve treatment options, we conducted a high-throughput screen to uncover compounds that block SARS-CoV-2 infection. A minimally pathogenic human betacoronavirus (OC43) was used to infect physiologically-relevant human pulmonary fibroblasts (MRC5) to facilitate rapid antiviral discovery in a preclinical model. Comprehensive profiling was conducted on more than 600 compounds, with each compound arrayed across 10 dose points. Our screening revealed several FDA-approved agents that can attenuate both OC43 and SARS-CoV-2 viral replication, including lapatinib, doramapimod, and 17-AAG. Importantly, lapatinib inhibited SARS-CoV-2 RNA replication by over 50,000-fold. Further, both lapatinib and doramapimod could be combined with remdesivir to improve antiviral activity in cells. These findings reveal novel therapeutic avenues that could limit SARS-CoV-2 infection.
Raymonda, M. H.、Ciesla, J. H.、Monaghan, M.、Leach, J.、Asantewaa, G.、Smorodintsev-Schiller, L. A.、Lutz, M. M.、Schafer, X. L.、Takimoto, T.、Dewhurst, S.、Munger, J.、Harris, I. S.
NSTL
Elsevier
