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dc.contributor.authorSong, Jiasheng
dc.contributor.authorClagett-Dame, Margaret
dc.contributor.authorPeterson, Richard E.
dc.contributor.authorHahn, Mark E.
dc.contributor.authorWestler, William M.
dc.contributor.authorSicinski, Rafal R.
dc.contributor.authorDeLuca, Hector F.
dc.date.accessioned2006-04-20T12:51:17Z
dc.date.available2006-04-20T12:51:17Z
dc.date.issued2002-10-30
dc.identifier.citationProceedings of the National Academy of Sciences 99 (2002): 14694-14699en
dc.identifier.urihttp://hdl.handle.net/1912/890
dc.descriptionAuthor Posting. © National Academy of Sciences, 2002. This article is posted here by permission of National Academy of Sciences for personal use, not for redistribution. The definitive version was published in Proceedings of the National Academy of Sciences 99 (2002): 14694-14699, doi:10.1073/pnas.232562899.en
dc.description.abstractThe aryl hydrocarbon receptor (AHR) is a ligand-inducible transcription factor that is best known because it mediates the actions of polycyclic and halogenated aromatic hydrocarbon environmental toxicants such as 3-methylcholanthrene and 2,3,7,8-tetrachlorodibenzo-p-dioxin. We report here the successful identification of an endogenous ligand for this receptor; {approx}20 µg was isolated in pure form from 35 kg of porcine lung. Its structure was deduced as 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester from extensive physical measurements and quantum mechanical calculations. In a reporter gene assay, this ligand activates the AHR with a potency five times greater than that of {beta}-naphthoflavone, a prototypical synthetic AHR ligand. 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester competes with 2,3,7,8-[3H]tetrachlorodibenzo-p-dioxin for binding to human, murine, and fish AHRs, thus showing that AHR activation is caused by direct receptor binding, and that recognition of this endogenous ligand is conserved from early vertebrates (fish) to humans.en
dc.description.sponsorshipThis work was supported by the Wisconsin Alumni Research Foundation, the University of Wisconsin Sea Grant Institute, and the National Institutes of Health.en
dc.format.extent334887 bytes
dc.format.mimetypeapplication/pdf
dc.language.isoen_USen
dc.publisherNational Academy of Sciencesen
dc.relation.urihttp://dx.doi.org/10.1073/pnas.232562899
dc.titleA ligand for the aryl hydrocarbon receptor isolated from lungen
dc.typeArticleen
dc.identifier.doi10.1073/pnas.232562899


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