Article
An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations.
Science translational medicine - 13 Mar 2024
Westberg Michael, Su Yichi, Zou Xinzhi, Huang Pinghan, Rustagi Arjun, Garhyan Jaishree, Patel Puja Bhavesh, Fernandez Daniel, Wu Yan, Hao Chenzhou, Lo Chieh-Wen, Karim Marwah, Ning Lin, Beck Aimee, Saenkham-Huntsinger Panatda, Tat Vivian, Drelich Aleksandra, Peng Bi-Hung, Einav Shirit, Tseng Chien-Te K, Blish Catherine, Lin Michael Z
Abstract excerpt
Inhibitors of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (Mpro) such as nirmatrelvir (NTV) and ensitrelvir (ETV) have proven effective in reducing the severity of COVID-19, but the presence of resistance-conferring mutations in sequenced viral genomes raises concerns about future drug resistance. Second-generation oral drugs that retain function against these mutants are thus...
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