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dc.contributor.author이공주-
dc.date.accessioned2016-08-29T11:08:50Z-
dc.date.available2016-08-29T11:08:50Z-
dc.date.issued2009-
dc.identifier.issn0006-2960-
dc.identifier.otherOAK-5776-
dc.identifier.urihttp://dspace.ewha.ac.kr/handle/2015.oak/232003-
dc.description.abstractN-Tosyl- L-phenylalanine chloromethyl ketone (TPCK), a serine/cysteine protease inhibitor, has been reported to inhibit expression of inflammatory mediators by blocking nuclear factor-κB (NF-κB) activation. We examined the effect of TPCK on the NF-κB activation pathway in HeLa cells by measuring the activity of IκB kinase (IKK) and p65/RelA-DNA binding. TPCK inhibited tumor necrosis factor-R-induced IKK activation and directly blocked IKK activity in vitro. TPCK-induced inhibition of NF-κB and IKK activation was abrogated by addition of the thiol-reducing agent dithiothreitol, suggesting that the effect of TPCK occurred through modification of a thiol group in IKK. Consistent with this, an IKKβ mutant in which Cys-179 was substituted with alanine was not more susceptible to TPCK. Our result also showed that TPCK inhibits the DNA binding of transiently expressed p65/RelA in HeLa cells. Inhibition of p65/RelA-DNA binding was recovered in the presence of dithiothreitol, and substitution of Cys-38 with Ser in p65/RelA rendered the protein resistant to inhibition by TPCK. Mass spectrometry analysis of IKKβ and p65/RelA isolated from cells treated with TPCK by UPLC-ESI-Q-TOF tandem MS revealed the labeling of Cys-179 of IKKβ and Cys-38 of p65/RelA with a tosylphenylalanylmethyl group. These results suggest that TPCK inhibits NF-κB activation by directly modifying thiol groups on two different targets: Cys-179 of IKKβ and Cys-38 of p65/RelA. ©2009 American Chemical Society.-
dc.languageEnglish-
dc.titleN-Tosyl-L-phenylalanine chloromethyl ketone inhibits NF-κB activation by blocking specific cysteine residues of IκB kinase β and p65/RelA-
dc.typeArticle-
dc.relation.issue30-
dc.relation.volume48-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.startpage7271-
dc.relation.lastpage7278-
dc.relation.journaltitleBiochemistry-
dc.identifier.doi10.1021/bi900660f-
dc.identifier.wosidWOS:000268231800020-
dc.identifier.scopusid2-s2.0-70350717978-
dc.author.googleHa K.-H.-
dc.author.googleByun M.-S.-
dc.author.googleChoi J.-
dc.author.googleJeong J.-
dc.author.googleLee K.-J.-
dc.author.googleJue D.-M.-
dc.contributor.scopusid이공주(7501497635)-
dc.date.modifydate20200221081000-
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약학대학 > 약학과 > Journal papers
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