Structural basis for the inhibition of SARS-CoV-2 main protease by antineoplastic drug Carmofur
Luke William Guddat,
Posted 09 Apr 2020
bioRxiv DOI: 10.1101/2020.04.09.033233 (published DOI: 10.1038/s41594-020-0440-6)
Posted 09 Apr 2020
The antineoplastic drug Carmofur was shown to inhibit SARS-CoV-2 main protease (Mpro). Here the X-ray crystal structure of Mpro in complex with Carmofur reveals that the carbonyl reactive group of Carmofur is covalently bound to catalytic Cys145, whereas its fatty acid tail occupies the hydrophobic S2 subsite. Carmofur inhibits viral replication in cells (EC50 = 24.30 μM) and it is a promising lead compound to develop new antiviral treatment for COVID-19. ### Competing Interest Statement The authors have declared no competing interest.
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