DC Field | Value | Language |
---|---|---|
dc.contributor.author | Park, SK | ko |
dc.contributor.author | Han, SB | ko |
dc.contributor.author | Lee, K | ko |
dc.contributor.author | Lee, HJ | ko |
dc.contributor.author | Kho, YH | ko |
dc.contributor.author | Chun, H | ko |
dc.contributor.author | Choi, Y | ko |
dc.contributor.author | Yang, JY | ko |
dc.contributor.author | Yoon, YD | ko |
dc.contributor.author | Lee, CW | ko |
dc.contributor.author | Kim, HM | ko |
dc.contributor.author | Choi, HM | ko |
dc.contributor.author | Tae, HS | ko |
dc.contributor.author | Lee, Hee Yoon | ko |
dc.contributor.author | Nam, KY | ko |
dc.contributor.author | Han, G | ko |
dc.date.accessioned | 2013-03-06T13:38:03Z | - |
dc.date.available | 2013-03-06T13:38:03Z | - |
dc.date.created | 2012-02-06 | - |
dc.date.created | 2012-02-06 | - |
dc.date.issued | 2006-03 | - |
dc.identifier.citation | BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, v.341, no.2, pp.627 - 634 | - |
dc.identifier.issn | 0006-291X | - |
dc.identifier.uri | http://hdl.handle.net/10203/87134 | - |
dc.description.abstract | The hydroxamic acid analogues (2) of the natural product gelastatins (1) were prepared by I step conversion reaction. The synthetic analogues (2) showed potent enzymatic inhibitory activities against MMP-2, MMP-9, and TACE IC50's of 6, 23, and 28 nM, respectively. In addition, 2 were able to inhibit TNF-alpha production effectively in mice as well as in a macrophage cell line, RAW 264.7. The protective effect of 2 also was examined on LPS-induced acute septic shock model. The mechanism of TNF-alpha inhibition was examined by RT-PCR and Western blot analyses. The relation of TACE and alpha-secretase was examined Using cellular alpha-secretase assays on IMR-32 and SH-SY5Y cell lines. The docking mode of 2 with the catalytic domain of TACE was illustrated to analyze the binding mode For the further analogue design. (c) 2006 Elsevier Inc. All rights reserved. | - |
dc.language | English | - |
dc.publisher | ACADEMIC PRESS INC ELSEVIER SCIENCE | - |
dc.subject | NECROSIS-FACTOR-ALPHA | - |
dc.subject | RHEUMATOID-ARTHRITIS | - |
dc.subject | TACE INHIBITORS | - |
dc.subject | CATALYTIC DOMAIN | - |
dc.subject | DISCOVERY | - |
dc.subject | DESIGN | - |
dc.subject | P1&apos | - |
dc.subject | DISINTEGRIN | - |
dc.subject | STRATEGIES | - |
dc.subject | PRECURSOR | - |
dc.title | Gelastatins and their hydroxamates as dual functional inhibitors for TNF-alpha converting enzyme and matrix metalloproteinases: Synthesis, biological evaluation, and mechanism studies | - |
dc.type | Article | - |
dc.identifier.wosid | 000235414400049 | - |
dc.identifier.scopusid | 2-s2.0-31444452901 | - |
dc.type.rims | ART | - |
dc.citation.volume | 341 | - |
dc.citation.issue | 2 | - |
dc.citation.beginningpage | 627 | - |
dc.citation.endingpage | 634 | - |
dc.citation.publicationname | BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | - |
dc.identifier.doi | 10.1016/j.bbrc.2005.12.219 | - |
dc.contributor.localauthor | Lee, Hee Yoon | - |
dc.contributor.nonIdAuthor | Park, SK | - |
dc.contributor.nonIdAuthor | Han, SB | - |
dc.contributor.nonIdAuthor | Lee, K | - |
dc.contributor.nonIdAuthor | Lee, HJ | - |
dc.contributor.nonIdAuthor | Kho, YH | - |
dc.contributor.nonIdAuthor | Chun, H | - |
dc.contributor.nonIdAuthor | Choi, Y | - |
dc.contributor.nonIdAuthor | Yang, JY | - |
dc.contributor.nonIdAuthor | Yoon, YD | - |
dc.contributor.nonIdAuthor | Lee, CW | - |
dc.contributor.nonIdAuthor | Kim, HM | - |
dc.contributor.nonIdAuthor | Choi, HM | - |
dc.contributor.nonIdAuthor | Tae, HS | - |
dc.contributor.nonIdAuthor | Nam, KY | - |
dc.contributor.nonIdAuthor | Han, G | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | tumor necrosis factor alpha | - |
dc.subject.keywordAuthor | inhibitors | - |
dc.subject.keywordAuthor | TNF alpha converting enzyme | - |
dc.subject.keywordAuthor | alpha-secretase | - |
dc.subject.keywordPlus | NECROSIS-FACTOR-ALPHA | - |
dc.subject.keywordPlus | RHEUMATOID-ARTHRITIS | - |
dc.subject.keywordPlus | TACE INHIBITORS | - |
dc.subject.keywordPlus | CATALYTIC DOMAIN | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | P1&apos | - |
dc.subject.keywordPlus | DISINTEGRIN | - |
dc.subject.keywordPlus | STRATEGIES | - |
dc.subject.keywordPlus | PRECURSOR | - |
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