KR33426, [2-(2,5-dichlorophenyl)-5-methyloxazol-4yl]carbonylguanidine, is a novel compound to be effective on mouse systemic lupus erythematosus
DC Field | Value | Language |
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dc.contributor.author | Lee, Geun-Hee | - |
dc.contributor.author | Oh, Jin-Mi | - |
dc.contributor.author | Kim, Hyun-Sun | - |
dc.contributor.author | Yoon, Won-Kee | - |
dc.contributor.author | Yi, Kyu Yang | - |
dc.contributor.author | Yang, Young | - |
dc.contributor.author | Han, Seung-Hyun | - |
dc.contributor.author | Lee, Sunkyung | - |
dc.contributor.author | Moon, Eun-Yi | - |
dc.date.available | 2021-02-22T13:16:09Z | - |
dc.date.issued | 2011-10 | - |
dc.identifier.issn | 0014-2999 | - |
dc.identifier.issn | 1879-0712 | - |
dc.identifier.uri | https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/12472 | - |
dc.description.abstract | B cell-activating factor (BAFF) is a key regulator of B lymphocyte development. Signals from BAFF are transmitted through binding to a specific BAFF receptor (BAFF-R). Here, we established screening method to find a specific inhibitor for the interference of BAFF-BAFF-R interactions. We screened oxazole-4-carbonylguanidine derivatives and selected KR33426, [2-(2,5-dichlorophenyl)-5-methyloxazol-4yl]carbonylguanidine, as a candidate to interfere BAFF-BAFF-R interactions. KR33426 inhibited BAFF-mediated anti-apoptotic effect on splenocytes as judged by hypodiploid cell formation. KR33426 also increased the degradation of procaspase-3 that was inhibited by BAFF protein. In addition, we examined whether KR33426 was effective on the treatment of systemic lupus erythematosus-like symptom in MRLlpr/lpr mouse. When 5 or 10 mg/kg KR33426 was intraperitoneally administered to MRLlpr/lpr mice for 4 weeks, histopathological changes were ameliorated in the narrowed space between renal glomerulus and glomerulus capsule. KR33426 reduced B220(+) B cell population and B cell mitogen, lipopolysaccharide-stimulated lymphocyte proliferation in splenocytes. KR33426 attenuated an increase in CD43(-)IgM(+) immature pro-B and a decrease in CD21(+) IgM(+) T2-B and IgD(+) IgM(-)recirculating-B cells on B cell development. Data show that KR33426 inhibits BAFF-BAFF-R interactions and it is effective on the treatment of systemic lupus erythematosus-like symptom in MRLlpr/lpr mice. Thus, it suggests that KR33426 is a novel candidate to develop anti-autoimmune therapeutics by the interference of BAFF-BAFF-R interactions, specifically. Crown Copyright (C) 2011 Published by Elsevier B.V. All rights reserved. | - |
dc.format.extent | 8 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | ELSEVIER SCIENCE BV | - |
dc.title | KR33426, [2-(2,5-dichlorophenyl)-5-methyloxazol-4yl]carbonylguanidine, is a novel compound to be effective on mouse systemic lupus erythematosus | - |
dc.type | Article | - |
dc.publisher.location | 네델란드 | - |
dc.identifier.doi | 10.1016/j.ejphar.2011.07.026 | - |
dc.identifier.scopusid | 2-s2.0-80053566491 | - |
dc.identifier.wosid | 000296411500014 | - |
dc.identifier.bibliographicCitation | EUROPEAN JOURNAL OF PHARMACOLOGY, v.668, no.3, pp 459 - 466 | - |
dc.citation.title | EUROPEAN JOURNAL OF PHARMACOLOGY | - |
dc.citation.volume | 668 | - |
dc.citation.number | 3 | - |
dc.citation.startPage | 459 | - |
dc.citation.endPage | 466 | - |
dc.type.docType | Article | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.subject.keywordPlus | CELL-ACTIVATING FACTOR | - |
dc.subject.keywordPlus | B-CELLS | - |
dc.subject.keywordPlus | FACTOR BAFF | - |
dc.subject.keywordPlus | AUTOIMMUNE-DISEASE | - |
dc.subject.keywordPlus | SURVIVAL FACTOR | - |
dc.subject.keywordPlus | TACI-IG | - |
dc.subject.keywordPlus | MICE | - |
dc.subject.keywordPlus | RECEPTOR | - |
dc.subject.keywordPlus | APRIL | - |
dc.subject.keywordPlus | ASTHMA | - |
dc.subject.keywordAuthor | BAFF | - |
dc.subject.keywordAuthor | KR33426 | - |
dc.subject.keywordAuthor | Carbonylguanidine derivative | - |
dc.subject.keywordAuthor | B cell | - |
dc.subject.keywordAuthor | Systemic lupus erythematosus | - |
dc.identifier.url | https://www.sciencedirect.com/science/article/abs/pii/S0014299911008016?via%3Dihub | - |
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