ArticleBioorganic & medicinal chemistry2008
Design, synthesis, and evaluation of 3C protease inhibitors as anti-enterovirus 71 agents.
Article in Bioorganic & medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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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.
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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
46 citing papers in PubMed, 88 citations in OpenAlex.
- Production of virus-like particles of FMDV by 3C protease cleaving precursor polyprotein P1 in vitro.Applied microbiology and biotechnology · 2024Article
- A Structural Investigation of the Interaction between a GC-376-Based Peptidomimetic PROTAC and Its Precursor with the Viral Main Protease of Coxsackievirus B3.Biomolecules · 2024Article
- Potent small molecule inhibitors against the 3C protease of foot-and-mouth disease virus.Microbiology spectrum · 2024Article
- PRSC chemical biology · 2023Review
- Computational and experimental studies of salvianolic acid A targets 3C protease to inhibit enterovirus 71 infection.Frontiers in pharmacology · 2023Article
- Beyond the vaccines: a glance at the small molecule and peptide-based anti-COVID19 arsenal.Journal of biomedical science · 2022Review
- Computational Screening of Newly Designed Compounds against Coxsackievirus A16 and Enterovirus A71.Molecules (Basel, Switzerland) · 2022Article
- Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLEuropean journal of medicinal chemistry · 2022Article
- Molecular docking study of variousFrontiers in microbiology · 2022Article
- 4-Iminooxazolidin-2-One as a Bioisostere of Cyanohydrin Suppresses EV71 Proliferation by Targeting 3CMicrobiology spectrum · 2021Article
- Janus All-Cis 2,3,4,5,6-Pentafluorocyclohexyl Building Blocks Applied to Medicinal Chemistry and Bioactives Discovery Chemistry.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Synthetic and computational efforts towards the development of peptidomimetics and small-molecule SARS-CoV 3CLpro inhibitors.Bioorganic & medicinal chemistry · 2021Review
- Innate immune evasion mediated by picornaviral 3C protease: Possible lessons for coronaviral 3C-like protease?Reviews in medical virology · 2021Review
- The Alpha Keto Amide Moiety as a Privileged Motif in Medicinal Chemistry: Current Insights and Emerging Opportunities.Journal of medicinal chemistry · 2021Review
- Recent advances of enterovirus 71Virology journal · 2020Review
- The Function and Mechanism of Enterovirus 71 (EV71) 3C Protease.Current microbiology · 2020Review
- Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease.Cell research · 2020Article
- Boceprevir, GC-376, and calpain inhibitors II, XII inhibit SARS-CoV-2 viral replication by targeting the viral main protease.bioRxiv : the preprint server for biology · 2020Article
- Antivirals and vaccines for Enterovirus A71.Journal of biomedical science · 2019Review
- Biochemical characterization of recombinant Avihepatovirus 3C protease and its localization.Virology journal · 2019Article
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Human enterovirus (EV) belongs to the picornavirus family, which consists of over 200 medically relevant viruses. A peptidomimetic inhibitor AG7088 was developed to inhibit the 3C protease of rhinovirus (a member of the family), a chymotrypsin-like protease required for viral replication, by forming a covalent bond with the active site Cys residue. In this study, we have prepared the recombinant 3C protease from EV71 (TW/2231/98), a particular strain which causes severe outbreaks in Asia, and developed inhibitors against the protease and the viral replication. For inhibitor design, the P3 group of AG7088, which is not interacting with the rhinovirus protease, was replaced with a series of cinnamoyl derivatives directly linked to P2 group through an amide bond to simplify the synthesis. While the replacement caused decreased potency, the activity can be largely improved by substituting the alpha,beta-unsaturated ester with an aldehyde at the P1' position. The best inhibitor 10b showed EC(50) of 18 nM without apparent toxicity (CC(50)>25 microM). Our study provides potent inhibitors of the EV71 3C protease as anti-EV71 agents and facilitates the combinatorial synthesis of derivatives for further improving the inhibitory activity.
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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.