Abstract
To test the effect of ligand flexibility on the selective transcriptional activities of ERalpha and ERbeta from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERalpha than with ERbeta, mimicking 4-hydroxytamoxifen more than raloxifene.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Estrogen Antagonists / chemistry
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Estrogen Antagonists / metabolism*
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Estrogen Receptor alpha
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Estrogen Receptor beta
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HeLa Cells
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Humans
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Ligands
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Raloxifene Hydrochloride / chemistry
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Raloxifene Hydrochloride / metabolism*
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Receptors, Estrogen / chemistry
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Receptors, Estrogen / metabolism*
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Tamoxifen / chemistry
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Tamoxifen / metabolism*
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Transcription Factor AP-1 / metabolism*
Substances
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Estrogen Antagonists
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Estrogen Receptor alpha
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Estrogen Receptor beta
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Ligands
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Receptors, Estrogen
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Transcription Factor AP-1
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Tamoxifen
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Raloxifene Hydrochloride