ArticleDrug design, development and therapy2015
Identification of covalent active site inhibitors of dengue virus protease.
Article in Drug design, development and therapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
13 citing papers in PubMed, 31 citations in OpenAlex.
- Achievements and Approaches in the Search for Small-Molecule Dengue NS2B/NS3 Inhibitors.Current medicinal chemistry · 2026Review
- A Non-Active-Site Inhibitor with Selectivity for Zika Virus NS2B-NS3 Protease.ACS infectious diseases · 2024Article
- Identification and In Silico Binding Study of a Highly Potent DENV NS2B-NS3 Covalent Inhibitor.ACS medicinal chemistry letters · 2022Article
- A short survey of dengue protease inhibitor development in the past 6 years (2015-2020) with an emphasis on similarities between DENV and SARS-CoV-2 proteases.Bioorganic & medicinal chemistry · 2021Review
- Structure and Dynamics of Zika Virus Protease and Its Insights into Inhibitor Design.Biomedicines · 2021Review
- Targeting the protease of West Nile virus.RSC medicinal chemistry · 2021Review
- Covalent Antiviral Agents.Advances in experimental medicine and biology · 2021Review
- Mechanisms of Action for Small Molecules Revealed by Structural Biology in Drug Discovery.International journal of molecular sciences · 2020Review
- Insights into Structures and Dynamics of Flavivirus Proteases from NMR Studies.International journal of molecular sciences · 2020Review
- Proteases from dengue, West Nile and Zika viruses as drug targets.Biophysical reviews · 2019Review
- Strategies Towards Protease Inhibitors for Emerging Flaviviruses.Advances in experimental medicine and biology · 2018Review
- Increased activity of unlinked Zika virus NS2B/NS3 protease compared to linked Zika virus protease.Biochemical and biophysical research communications · 2017Article
- Anti-dengue drug: viral polyprotein, a potential target.Drug design, development and therapy · 2016Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
14 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Dengue virus (DENV) protease is an attractive target for drug development; however, no compounds have reached clinical development to date. In this study, we utilized a potent West Nile virus protease inhibitor of the pyrazole ester derivative class as a chemical starting point for DENV protease drug development. Compound potency and selectivity for DENV protease were improved through structure-guided small molecule optimization, and protease-inhibitor binding interactions were validated biophysically using nuclear magnetic resonance. Our work strongly suggests that this class of compounds inhibits flavivirus protease through targeted covalent modification of active site serine, contrary to an allosteric binding mechanism as previously described.
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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.