Identification of Diaryl-Quinoline Compounds as Entry Inhibitors of Ebola Virus

Cui, Qinghua; Cheng, Han; Xiong, Rui; Zhang, Gang; Du, Ruikun; Anantpadma, Manu; Davey, Robert A.; Rong, Lijun

doi:10.3390/v10120678

Cited by 29 publications

(22 citation statements)

References 43 publications

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“…These secondary hits may potentially target other steps rather than RNA replication/transcription in the influenza virus replication cycle. Of note, cytotoxic compounds and luciferase inhibitors might also be initially identified as shared “hits”, where “toxic hits” can be excluded by a toxicity screening, while an orthogonal counterscreen using wild-type IAVs can exclude the small molecules that inhibit luciferase activity [40].…”

Section: Resultsmentioning

confidence: 99%

A Parallel Phenotypic Versus Target-Based Screening Strategy for RNA-Dependent RNA Polymerase Inhibitors of the Influenza A Virus

Zhao

Wang

Cui

et al. 2019

Viruses

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Influenza A virus infections cause significant morbidity and mortality, and novel antivirals are urgently needed. Influenza RNA-dependent RNA polymerase (RdRp) activity has been acknowledged as a promising target for novel antivirals. In this study, a phenotypic versus target-based screening strategy was established to identify the influenza A virus inhibitors targeting the virus RNA transcription/replication steps by sequentially using an RdRp-targeted screen and a replication-competent reporter virus-based approach using the same compounds. To demonstrate the utility of this approach, a pilot screen of a library of 891 compounds derived from natural products was carried out. Quality control analysis indicates that the primary screen was robust for identification of influenza A virus inhibitors targeting RdRp activity. Finally, two hit candidates were identified, and one was validated as a putative RdRp inhibitor. This strategy can greatly reduce the number of false positives and improve the accuracy and efficacy of primary screening, thereby providing a powerful tool for antiviral discovery.

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Section: Resultsmentioning

confidence: 99%

A Parallel Phenotypic Versus Target-Based Screening Strategy for RNA-Dependent RNA Polymerase Inhibitors of the Influenza A Virus

Zhao

Wang

Cui

et al. 2019

Viruses

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“…Recently, Cui and co-workers reported that diaryl-quinoline compounds are also active as entry inhibitors of EBOV [112].…”

Section: Ebola Virus Entry Inhibitorsmentioning

confidence: 99%

Ebola Virus Entry: From Molecular Characterization to Drug Discovery

Salata

Calistri

Alvisi

et al. 2019

Viruses

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Ebola Virus Disease (EVD) is one of the most lethal transmissible infections, characterized by a high fatality rate, and caused by a member of the Filoviridae family. The recent large outbreak of EVD in Western Africa (2013–2016) highlighted the worldwide threat represented by the disease and its impact on global public health and the economy. The development of highly needed anti-Ebola virus antivirals has been so far hampered by the shortage of tools to study their life cycle in vitro, allowing to screen for potential active compounds outside a biosafety level-4 (BSL-4) containment. Importantly, the development of surrogate models to study Ebola virus entry in a BSL-2 setting, such as viral pseudotypes and Ebola virus-like particles, tremendously boosted both our knowledge of the viral life cycle and the identification of promising antiviral compounds interfering with viral entry. In this context, the combination of such surrogate systems with large-scale small molecule compounds and haploid genetic screenings, as well as rational drug design and drug repurposing approaches will prove priceless in our quest for the development of a treatment for EVD.

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“…Recently, Cui and co-workers reported that diaryl-quinoline compounds are also active as entry inhibitors of EBOV [109].…”

Section: Miscellaneous Compounds That Inhibit Ebov Entrymentioning

confidence: 99%

Ebolavirus Entry: From Molecular Characterization to Drug Discovery

Salata¹,

Calistri²,

Alvisi³

et al. 2019

Preprint

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Ebola Virus Disease (EVD) is one of the most lethal transmissible infections characterized by a high fatality rate, and caused by members of the Filoviridae family. The recent large outbreak of EVD in West Africa (2013-2016), highlighted the worldwide danger of this disease and its impact on global public health and economy. The development of highly needed anti-Filoviridae antivirals has been so far hampered by the shortage of tools to study their life cycle in vitro, and therefore screen for potential active compounds outside a biosafety level-4 (BSL-4) containment. Importantly, the development of surrogate models to in vitro study of Filoviridae entry in a BSL-2 setting, such as viral pseudotypes and Ebola virus like particles, tremendously boosted both our knowledge on viral life cycle and the identification of promising anti-Filoviridae compounds interfering with viral entry. In this context, the combination of such surrogate systems with large-scale small molecule compounds and haploid genetic screenings, as well as rational drug design and drug repurposing approaches will prove priceless in our quest for the development of a treatment for EVD.

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Identification of Diaryl-Quinoline Compounds as Entry Inhibitors of Ebola Virus

Cited by 29 publications

References 43 publications

A Parallel Phenotypic Versus Target-Based Screening Strategy for RNA-Dependent RNA Polymerase Inhibitors of the Influenza A Virus

A Parallel Phenotypic Versus Target-Based Screening Strategy for RNA-Dependent RNA Polymerase Inhibitors of the Influenza A Virus

Ebola Virus Entry: From Molecular Characterization to Drug Discovery

Ebolavirus Entry: From Molecular Characterization to Drug Discovery

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