Development of curcumin-based amyloid β aggregation inhibitors for Alzheimer's disease using the SAR matrix approach

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dc.contributor.authorR Y Utomo-
dc.contributor.authorY Asawa-
dc.contributor.authorS Okada-
dc.contributor.authorHyun Seung Ban-
dc.contributor.authorA Yoshimori-
dc.contributor.authorJ Bajorath-
dc.contributor.authorH Nakamura-
dc.date.accessioned2021-08-17T15:30:24Z-
dc.date.available2021-08-17T15:30:24Z-
dc.date.issued2021-
dc.identifier.issn0968-0896-
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/24640-
dc.description.abstractAmyloid β (Aβ) aggregation inhibitor activity cliff involving a curcumin structure was predicted using the SAR Matrix method on the basis of 697 known Aβ inhibitors from ChEMBL (data set 2487). Among the compounds predicted, compound B was found to possess approximately 100 times higher inhibitory activity toward Aβ aggregation than curcumin. TEM images indicate that compound B induced the shortening of Aβ fibrils and increased the generation of Aβ oligomers in a concentration dependent manner. Furthermore, compound K, in which the methyl ester of compound B was replaced by the tert-butyl ester, possessed low cytotoxicity on N2A cells and attenuated Aβ-induced cytotoxicity, indicating that compound K would have an ability for preventing neurotoxicity caused by Aβ aggregation.-
dc.publisherElsevier-
dc.titleDevelopment of curcumin-based amyloid β aggregation inhibitors for Alzheimer's disease using the SAR matrix approach-
dc.title.alternativeDevelopment of curcumin-based amyloid β aggregation inhibitors for Alzheimer's disease using the SAR matrix approach-
dc.typeArticle-
dc.citation.titleBioorganic & Medicinal Chemistry-
dc.citation.number0-
dc.citation.endPage116357-
dc.citation.startPage116357-
dc.citation.volume46-
dc.contributor.affiliatedAuthorHyun Seung Ban-
dc.contributor.alternativeNameUtomo-
dc.contributor.alternativeNameAsawa-
dc.contributor.alternativeNameOkada-
dc.contributor.alternativeName반현승-
dc.contributor.alternativeNameYoshimori-
dc.contributor.alternativeNameBajorath-
dc.contributor.alternativeNameNakamura-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry, vol. 46, pp. 116357-116357-
dc.identifier.doi10.1016/j.bmc.2021.116357-
dc.subject.keywordSAR matrix-
dc.subject.keywordCurcumin-
dc.subject.keywordAmyloid β-
dc.subject.keywordAlzheimer’s disease-
dc.subject.keywordNeurotoxicity-
dc.subject.localSAR matrix-
dc.subject.localCurcumin-
dc.subject.localcurcumin-
dc.subject.localAmyloid beta-
dc.subject.localAmyloid β-
dc.subject.localamyloid-β-
dc.subject.localAmyloid-beta-
dc.subject.localalzheimer's disease-
dc.subject.localAlzheimer’s disease (AD)-
dc.subject.localAlzheimer’s disease-
dc.subject.localAlzheimer's Disease-
dc.subject.localAlzheimer disease-
dc.subject.localAlzheimer's disease (AD)-
dc.subject.localAlzheimer′s disease-
dc.subject.localAlzheimer's disease-
dc.subject.localNeurotoxicity-
dc.subject.localneurotoxicity-
dc.description.journalClassY-
Appears in Collections:
Division of Biomedical Research > Biotherapeutics Translational Research Center > 1. Journal Articles
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