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

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An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Identification of Diaryl-Quinoline Compounds as Entry Inhibitors of Ebola Virus
Creator	Cheng, Han Rong, Lijun Zhang, Gang Anantpadma, Manu Cui, Qinghua Du, Ruikun Xiong, Rui Davey, Robert
Source	PMC
abstract	Ebola virus is the causative agent of Ebola virus disease in humans. The lethality of Ebola virus infection is about 50%, supporting the urgent need to develop anti-Ebola drugs. Glycoprotein (GP) is the only surface protein of the Ebola virus, which is functionally critical for the virus to attach and enter the host cells, and is a promising target for anti-Ebola virus drug development. In this study, using the recombinant HIV-1/Ebola pseudovirus platform we previously established, we evaluated a small molecule library containing various quinoline compounds for anti-Ebola virus entry inhibitors. Some of the quinoline compounds specifically inhibited the entry of the Ebola virus. Among them, compound SYL1712 was the most potent Ebola virus entry inhibitor with an IC(50) of ~1 μM. The binding of SYL1712 to the vial glycoprotein was computationally modeled and was predicted to interact with specific residues of GP. We used the time of the addition assay to show that compound SYL1712 blocks Ebola GP-mediated entry. Finally, consistent with being an Ebola virus entry inhibitor, compound SYL1712 inhibited infectious Ebola virus replication in tissue culture under biosafety level 4 containment, with an IC(50) of 2 μM. In conclusion, we identified several related molecules with a diaryl-quinoline scaffold as potential anti-EBOV entry inhibitors, which can be further optimized for anti-Ebola drug development.
has issue date	2018-11-30(xsd:dateTime)
bibo:doi	10.3390/v10120678
bibo:pmid	30513600
has license	cc-by
sha1sum (hex)	eccc33ccb0e981e31f4d18d258274a7dae3ca2bc
schema:url	https://doi.org/10.3390/v10120678
resource representing a document's title	Identification of Diaryl-Quinoline Compounds as Entry Inhibitors of Ebola Virus
has PubMed Central identifier	PMC6315506
has PubMed identifier	30513600
schema:publication	Viruses
resource representing a document's body	covid:eccc33ccb0e981e31f4d18d258274a7dae3ca2bc#body_text
is schema:about of	named entity 'PREDICTED' named entity 'IS A' named entity 'ENTRY INHIBITORS' named entity 'EVALUATED' named entity 'HIV-1' named entity 'SMALL MOLECULE' named entity 'SUPPORTING' named entity 'NEED' named entity 'TARGET' named entity 'LIBRARY' named entity 'EBOLA VIRUS DISEASE' named entity 'COMPOUND' named entity 'HOST CELLS' named entity 'IS ABOUT' named entity 'QUINOLINE' named entity 'SPECIFIC' named entity 'DRUGS' named entity 'SURFACE PROTEIN' named entity 'HUMANS' named entity 'BEING' named entity 'CONTAINMENT' named entity 'ENTER' named entity 'VIAL' named entity 'EBOLA VIRUS' named entity 'host' named entity 'ENTRY INHIBITORS' named entity 'IDENTIFICATION' named entity 'PREVIOUSLY' named entity 'VIRUS ENTRY' named entity 'TISSUE CULTURE' named entity 'USING' named entity 'SCAFFOLD' named entity 'VARIOUS' named entity 'IDENTIFIED' named entity 'POTENTIAL' named entity 'ASSAY' named entity 'VIRUS REPLICATION' named entity 'CAUSATIVE AGENT' named entity 'TIME' named entity '50%' named entity 'LETHALITY' named entity 'URGENT' named entity 'RELATED' named entity 'QUINOLINE' named entity 'EBOLA VIRUS' named entity 'CRITICAL' named entity 'MEDIATED' named entity 'MODELED' named entity 'ATTACH' named entity 'CONTAINING' named entity 'ADDITION' named entity 'EBOLA VIRUS INFECTION' named entity 'BIOSAFETY LEVEL 4' named entity 'PLATFORM' named entity 'ESTABLISHED' named entity 'BINDING' named entity 'GLYCOPROTEIN' named entity 'VIRUS' named entity 'BLOCKS' named entity 'MOLECULES' named entity 'USED' named entity 'RECOMBINANT' named entity 'CONSISTENT WITH' named entity 'CONCLUSION' named entity 'INFECTIOUS' named entity 'VIRUS ENTRY INHIBITOR' named entity 'ENTRY' named entity 'EBOLA' named entity 'INHIBITED' named entity 'DRUG DEVELOPMENT' named entity 'PROTEIN ' named entity 'TO INTERACT WITH' named entity 'STUDY' named entity 'PSEUDOVIRUS'

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