Targeting the SARS CoV 2 Main Protease to Repurpose Drugs for COVID 19.

bioRxiv(2020)

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摘要
Guided by a computational docking analysis, about 30 FDA/EMA-approved small molecule medicines were characterized on their inhibition of the SARS-CoV-2 main protease (M). Of these tested small molecule medicines, six displayed an IC value in inhibiting M below 100 μM. Three medicines pimozide, ebastine, and bepridil are basic small molecules that are expected to exert a similar effect as hydroxychloroquine in raising endosomal pH for slowing down the SARS-CoV-2 entry into human cell hosts. Bepridil has been previously explored in a high dose as 100 mg/kg for treating diseases. Its high dose use will likely achieve dual functions in treating COVID-19 by both raising the endosomal pH to slow viral entry and inhibiting M in infected cells. Therefore, the current study urges serious considerations of using bepridil in COVID-19 clinical tests.
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关键词
COVID-19,SARS-CoV-2,bepridil,pimozide,ebastine
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