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Synthesis and structure–activity relationship study of saponin-based membrane fusion inhibitors against SARS-CoV-2

DC Field Value Language
dc.contributor.authorJang, Youngho-
dc.contributor.authorTai Young Kim-
dc.contributor.authorJeon, Sangeun-
dc.contributor.authorLim, Hyeonggeun-
dc.contributor.authorLee, JinAh-
dc.contributor.authorKim, Seungtaek-
dc.contributor.authorC. Justin Lee-
dc.contributor.authorHan, Sunkyu-
dc.date.accessioned2023-01-27T00:39:21Z-
dc.date.available2023-01-27T00:39:21Z-
dc.date.created2022-07-18-
dc.date.issued2022-10-
dc.identifier.issn0045-2068-
dc.identifier.urihttps://pr.ibs.re.kr/handle/8788114/12834-
dc.description.abstract© 2022 Elsevier Inc.We previously discovered that triterpenoid saponin platycodin D inhibits the SARS-CoV-2 entry to the host cell. Herein, we synthesized various saponin derivatives and established a structure–activity relationship of saponin-based antiviral agents against SARS-CoV-2. We discovered that the C3-glucose, the C28-oligosaccharide moiety that consist of (→3)-β-D-Xyl-(1 → 4)-α-L-Rham-(1 → 2)-β-D-Ara-(1 → ) as the last three sugar units, and the C16-hydroxyl group were critical components of saponin-based coronavirus cell entry inhibitors. These findings enabled us to develop minimal saponin-based antiviral agents that are equipotent to the originally discovered platycodin D. We found that our saponin-based antiviral agents inhibited both the endosomal and transmembrane protease serine 2-mediated cell surface viral entries. Cell fusion assay experiment revealed that our newly developed compounds inhibit the SARS-CoV-2 entry by blocking the fusion between the viral and host cell membranes. The effectiveness of the newly developed antiviral agents over various SARS-CoV-2 variants hints at the broad-spectrum antiviral efficacy of saponin-based therapeutics against future coronavirus variants.-
dc.language영어-
dc.publisherAcademic Press Inc.-
dc.titleSynthesis and structure–activity relationship study of saponin-based membrane fusion inhibitors against SARS-CoV-2-
dc.typeArticle-
dc.type.rimsART-
dc.identifier.wosid000841132200001-
dc.identifier.scopusid2-s2.0-85133550574-
dc.identifier.rimsid78501-
dc.contributor.affiliatedAuthorTai Young Kim-
dc.contributor.affiliatedAuthorC. Justin Lee-
dc.identifier.doi10.1016/j.bioorg.2022.105985-
dc.identifier.bibliographicCitationBioorganic Chemistry, v.127-
dc.relation.isPartOfBioorganic Chemistry-
dc.citation.titleBioorganic Chemistry-
dc.citation.volume127-
dc.type.docTypeArticle-
dc.description.journalClass1-
dc.description.journalClass1-
dc.description.isOpenAccessN-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.relation.journalResearchAreaBiochemistry & Molecular Biology-
dc.relation.journalResearchAreaChemistry-
dc.relation.journalWebOfScienceCategoryBiochemistry & Molecular Biology-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.subject.keywordAuthorComplex molecules synthesis-
dc.subject.keywordAuthorCOVID-19-
dc.subject.keywordAuthorMembrane fusion-
dc.subject.keywordAuthorSaponins-
dc.subject.keywordAuthorSARS-CoV-2-
Appears in Collections:
Center for Cognition and Sociality(인지 및 사회성 연구단) > 1. Journal Papers (저널논문)
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