ArticlePharmaceutical science advances2025
Assay development and screening of inhibitors targeting the SARS-CoV-2 2'-O-methyltransferase NSP16.
Article in Pharmaceutical science advances, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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The trial behind it
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Who cites it
2 citing papers in PubMed.
- Targeting SARS-CoV-2 Non-Structural Proteins: A Blueprint for Next-Generation Small-Molecule Coronavirus Antivirals.Pharmaceutics · 2026Review
- Selective Targeting of Protein Arginine Methyltransferase 1 (PRMT1) Mutant Activity by a Small Molecule Activation Strategy.ACS chemical biology · 2026Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
The coronavirus disease-2019 (COVID-19) pandemic, etiologically caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has profoundly impacted the global health. While vaccines have been developed, they have shown limited efficacy in treating patients already under infection or preventing infection with emerging SARS-CoV-2 variants. The nonstructural protein 16 (NSP16), with the assistance of the nonstructural protein 10 (NSP10), is responsible for forming the Cap-1 structure, which is critical for viral replication and immune evasion through the 5'-capping of viral mRNA. As a result, NSP16/NSP10 has emerged as a promising target for antiviral treatment of coronaviruses. In this study, we aimed to discover small molecule inhibitors of NSP16/NSP10 by leveraging recent structural insights and combined tools of virtual and experimental screenings. We designed a simple scintillation proximity assay to enable biochemical testing for NSP16/NSP10 enzymatic activity and applied it to screen inhibitors from candidate hit compounds that are derived from molecular docking-based virtual screenings. We identified potential hits that inhibit the NSP16 activity with cellular efficacy. Together with structural analysis and chemotype categorization, this study lays the groundwork for novel antiviral therapeutics development against SARS-CoV-2 and related coronaviruses.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.