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The COVID-19 pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) continually poses serious threats to global public health. The main protease (Mpro) of SARS-CoV-2 plays a central role in viral replication. We designed and synthesized 32 new bicycloproline-containing Mpro inhibitors derived from either boceprevir or telaprevir, both of which are approved antivirals. All compounds inhibited SARS-CoV-2 Mpro activity in vitro, with 50% inhibitory concentration values ranging from 7.6 to 748.5 nM. The cocrystal structure of Mpro in complex with MI-23, one of the most potent compounds, revealed its interaction mode. Two compounds (MI-09 and MI-30) showed excellent antiviral activity in cell-based assays. In a transgenic mouse model of SARS-CoV-2 infection, oral or intraperitoneal treatment with MI-09 or MI-30 significantly reduced lung viral loads and lung lesions. Both also displayed good pharmacokinetic properties and safety in rats.[/vc_column_text][vc_column_text]
In this study humanised ACE2 mice from GemPharmatech (strain ID, T037659) was used to study the effects of two antiviral compounds.
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10.1126/science.abf1611[/vc_column_text][/vc_column][/vc_row][vc_row][vc_column][vc_column_text]
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Shao, F., Liu, Q., Zhu, Y. et al. Targeting chondrocytes for arresting bony fusion in ankylosing spondylitis. Nat Commun 12, 6540 (2021). https://doi.org/10.1038/s41467-021-26750-6
Wu Q, Liang X, Wang K, et al. Intestinal hypoxia-inducible factor 2α regulates lactate levels to shape the gut microbiome and alter thermogenesis. Cell Metab. 2021;33(10):1988-2003.e7. doi:10.1016/j.cmet.2021.07.007
Li, Y., Lu, Y., Lin, SH. et al. Insulin signaling establishes a developmental trajectory of adipose regulatory T cells. Nat Immunol 22, 1175–1185 (2021). https://doi.org/10.1038/s41590-021-01010-3
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