ArticleJournal of enzyme inhibition and medicinal chemistry2021
Repurposing existing drugs: identification of SARS-CoV-2 3C-like protease inhibitors.
Article in Journal of enzyme inhibition and medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
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Who cites it
28 citing papers in PubMed, 44 citations in OpenAlex.
- Repurposing FDA-Approved Drugs as Potential Inhibitors of Feline Infectious Peritonitis Virus 3CLACS pharmacology & translational science · 2026Article
- An equivariant pretrained transformer for unified 3D molecular representation learning.Nature communications · 2026Article
- Glycosylated 18β-glycyrrhetinic acid derivatives as promising inhibitors of the SARS-CoV-2 main protease.RSC advances · 2025Article
- Tranylcypromine: a promising repurposed drug against Leishmaniases.Frontiers in microbiology · 2025Article
- The SARS-CoV-2 MACS synthetic biology · 2024Article
- A potential allosteric inhibitor of SARS-CoV-2 main protease (MFrontiers in molecular biosciences · 2024Article
- Structure and function of SARS-CoV and SARS-CoV-2 main proteases and their inhibition: A comprehensive review.European journal of medicinal chemistry · 2023Review
- Indole-Based Compounds as Potential Drug Candidates for SARS-CoV-2.Molecules (Basel, Switzerland) · 2023Review
- Ovatodiolide inhibits SARS-CoV-2 replication and ameliorates pulmonary fibrosis through suppression of the TGF-β/TβRs signaling pathway.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2023Article
- In Silico Screening of Drugs That Target Different Forms of E Protein for Potential Treatment of COVID-19.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Virtual high-throughput screening: Potential inhibitors targeting aminopeptidase N (CD13) and PIKfyve for SARS-CoV-2.Open life sciences · 2023Article
- Highlights on molecular targets in the management of COVID-19: Possible role of pharmacogenomics.The Journal of international medical research · 2023Review
- Systematic comparison of differential expression networks in MTB mono-, HIV mono- and MTB/HIV co-infections for drug repurposing.PLoS computational biology · 2022Article
- Acriflavine and proflavine hemisulfate as potential antivirals by targeting MBioorganic chemistry · 2022Article
- A new glimpse on the active site of SARS-CoV-2 3CLpro, coupled with drug repurposing study.Molecular diversity · 2022Article
- The SARS-CoV-2 main protease (MMedComm · 2022Review
- Saquinavir: From HIV to COVID-19 and Cancer Treatment.Biomolecules · 2022Review
- Characterization of raloxifene as a potential pharmacological agent against SARS-CoV-2 and its variants.Cell death & disease · 2022Article
- A VSV-based assay quantifies coronavirus Mpro/3CLpro/Nsp5 main protease activity and chemical inhibition.Communications biology · 2022Article
- Repurposing of Chemotherapeutics to Combat COVID-19.Current topics in medicinal chemistry · 2022Article
Corrections and comments
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Authors and funding
7 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for coronavirus disease 2019 (COVID-19). Since its emergence, the COVID-19 pandemic has not only distressed medical services but also caused economic upheavals, marking urgent the need for effective therapeutics. The experience of combating SARS-CoV and MERS-CoV has shown that inhibiting the 3-chymotrypsin-like protease (3CLpro) blocks the replication of the virus. Given the well-studied properties of FDA-approved drugs, identification of SARS-CoV-2 3CLpro inhibitors in an FDA-approved drug library would be of great therapeutic value. Here, we screened a library consisting of 774 FDA-approved drugs for potent SARS-CoV-2 3CLpro inhibitors, using an intramolecularly quenched fluorescence (IQF) peptide substrate. Ethacrynic acid, naproxen, allopurinol, butenafine hydrochloride, raloxifene hydrochloride, tranylcypromine hydrochloride, and saquinavir mesylate have been found to block the proteolytic activity of SARS-CoV-2 3CLpro. The inhibitory activity of these repurposing drugs against SARS-CoV-2 3CLpro highlights their therapeutic potential for treating COVID-19 and other Betacoronavirus infections.
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