DC Field | Value | Language |
---|---|---|
dc.contributor.author | Shin, Yongje | ko |
dc.contributor.author | Lim, Sang Min | ko |
dc.contributor.author | Yan, Hong Hua | ko |
dc.contributor.author | Jung, Sungwoo | ko |
dc.contributor.author | Fang, Zhenghuan | ko |
dc.contributor.author | Jung, Kyung Hee | ko |
dc.contributor.author | Hong, Soon-Sun | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.date.accessioned | 2016-12-01T04:44:57Z | - |
dc.date.available | 2016-12-01T04:44:57Z | - |
dc.date.created | 2016-11-16 | - |
dc.date.created | 2016-11-16 | - |
dc.date.issued | 2016-11 | - |
dc.identifier.citation | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.123, pp.544 - 556 | - |
dc.identifier.issn | 0223-5234 | - |
dc.identifier.uri | http://hdl.handle.net/10203/214413 | - |
dc.description.abstract | Targeting I kappa B kinase beta (IKK beta) can be a promising strategy in the development of a therapeutic treatment of inflammatory diseases because IKK beta is well-recognized as a key mediator of the NF-kappa B signaling pathway. In this study, we have successfully developed a structure-activity relationship (SAR) profile of the aminopyrimidine-based IKK beta inhibitors through the structure-based design strategy to improve the physicochemical properties and cellular activity in terms of the anti-inflammatory effects. Representative compounds exhibited desirable activity in nitric oxide (NO) reduction by inhibiting the synthesis of inducible nitric oxide synthase (iNOS), and strongly inhibited the expression of pro-inflammatory cytokines (IL-1 alpha, IL-6, and TNF-alpha). The inhibitory effects of 8e on the phosphorylation in the NF-kappa B pathway further supported that the suppression of the NF-kappa B signaling pathway induced the anti-inflammatory effect in LPS-stimulated Raw 264.7 cells. (C) 2016 Elsevier Masson SAS. All rights reserved | - |
dc.language | English | - |
dc.publisher | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER | - |
dc.title | Optimization and biological evaluation of aminopyrimidine-based I kappa B kinase beta inhibitors with potent anti-inflammatory effects | - |
dc.type | Article | - |
dc.identifier.wosid | 000385319000044 | - |
dc.identifier.scopusid | 2-s2.0-84982844988 | - |
dc.type.rims | ART | - |
dc.citation.volume | 123 | - |
dc.citation.beginningpage | 544 | - |
dc.citation.endingpage | 556 | - |
dc.citation.publicationname | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | - |
dc.identifier.doi | 10.1016/j.ejmech.2016.07.075 | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Lim, Sang Min | - |
dc.contributor.nonIdAuthor | Yan, Hong Hua | - |
dc.contributor.nonIdAuthor | Fang, Zhenghuan | - |
dc.contributor.nonIdAuthor | Jung, Kyung Hee | - |
dc.contributor.nonIdAuthor | Hong, Soon-Sun | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | IKK beta | - |
dc.subject.keywordAuthor | Inhibitor | - |
dc.subject.keywordAuthor | Structure-activity relationship | - |
dc.subject.keywordAuthor | NO reduction | - |
dc.subject.keywordAuthor | Anti-inflammatory effect | - |
dc.subject.keywordPlus | IKK-BETA | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | INFLAMMATION | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | VIVO | - |
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