ArticleJournal of biomolecular screening2011
A high-throughput screening assay for the identification of flavivirus NS5 capping enzyme GTP-binding inhibitors: implications for antiviral drug development.
Article in Journal of biomolecular screening, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 28 citations in OpenAlex.
- Development of a luminescence-based method for measuring West Nile Virus MTase activity and its application to screen for antivirals.Current research in microbial sciences · 2024Article
- Fused Tetrahydroquinolines Are Interfering with Your Assay.Journal of medicinal chemistry · 2023Review
- Enzymatic Assays to Explore Viral mRNA Capping Machinery.Chembiochem : a European journal of chemical biology · 2021Review
- Alkyne-Tagged Apigenin, a Chemical Tool to Navigate Potential Targets of Flavonoid Anti-Dengue Leads.Molecules (Basel, Switzerland) · 2021Article
- Flavivirus: From Structure to Therapeutics Development.Life (Basel, Switzerland) · 2021Review
- Flavivirus enzymes and their inhibitors.The Enzymes · 2021Article
- Direct High-Throughput Screening Assay for mRNA Cap Guanine-N7 Methyltransferase Activity.Chemistry (Weinheim an der Bergstrasse, Germany) · 2020Article
- Identification of small molecule inhibitors of the Chikungunya virus nsP1 RNA capping enzyme.Antiviral research · 2018Article
- Glutathionylation of dengue and Zika NS5 proteins affects guanylyltransferase and RNA dependent RNA polymerase activities.PloS one · 2018Article
- An Overview of Current Approaches Toward the Treatment and Prevention of West Nile Virus Infection.Methods in molecular biology (Clifton, N.J.) · 2016Article
- A Sensitive and Robust High-Throughput Screening Assay for Inhibitors of the Chikungunya Virus nsP1 Capping Enzyme.PloS one · 2016Article
- Article
- Murine Efficacy and Pharmacokinetic Evaluation of the Flaviviral NS5 Capping Enzyme 2-Thioxothiazolidin-4-One Inhibitor BG-323.PloS one · 2015Article
- West Nile virus drug discovery.Viruses · 2013Review
- The viral RNA capping machinery as a target for antiviral drugs.Antiviral research · 2012Review
- Identification of a novel antiviral inhibitor of the flavivirus guanylyltransferase enzyme.Journal of virology · 2012Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 1 country.
Funding
Abstract
There are no effective antivirals currently available for the treatment of flavivirus infection in humans. As such, the identification and characterization of novel drug target sites are critical to developing new classes of antiviral drugs. The flavivirus NS5 N-terminal capping enzyme (CE) is vital for the formation of the viral RNA cap structure, which directs viral polyprotein translation and stabilizes the 5' end of the viral genome. The structure of the flavivirus CE has been solved, and a detailed understanding of the CE-guanosine triphosphate (GTP) and CE-RNA cap interactions is available. Because of the essential nature of the interaction for viral replication, disrupting CE-GTP binding is an attractive approach for drug development. The authors have previously developed a robust assay for monitoring CE-GTP binding in real time. They adapted this assay for high-throughput screening and performed a pilot screen of 46 323 commercially available compounds. A number of small-molecule inhibitors capable of displacing a fluorescently labeled GTP in vitro were identified, and a second functional assay was developed to identify false positives. The results presented indicate that the flavivirus CE cap-binding site is a valuable new target site for antiviral drug discovery and should be further exploited for broad-spectrum anti-flaviviral drug development.
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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.