Differential ligand activation of estrogen receptors ERα and ERrβ at AP1 sites

Kolja Paech, Paul Webb, George G J M Kuiper, Stefan Nilsson, Jan Åke Gustafsson, Peter J. Kushner, Thomas (Tom) Scanlan

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Abstract

The transactivation properties of the two estrogen receptors, ERα and ERβ, were examined with different ligands in the context of an estrogen response element and an AP1 element. ERα and ERβ were shown to signal in opposite ways when complexed with the natural hormone estradiol from an AP1 site: with ERα, 17β-estradiol activated transcription, whereas with ERβ, 17β-estradiol inhibited transcription. Moreover, the antiestrogens tamoxifen, raloxifene, and Imperial Chemical Industries 164384 were potent transcriptional activators with ERβ at an AP1 site. Thus, the two ERs signal in different ways depending on ligand and response element. This suggests that ERα and ERβ may play different roles in gene regulation.

Original languageEnglish (US)
Pages (from-to)1508-1510
Number of pages3
JournalScience
Volume277
Issue number5331
DOIs
Publication statusPublished - Sep 5 1997
Externally publishedYes

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Paech, K., Webb, P., Kuiper, G. G. J. M., Nilsson, S., Gustafsson, J. Å., Kushner, P. J., & Scanlan, T. T. (1997). Differential ligand activation of estrogen receptors ERα and ERrβ at AP1 sites. Science, 277(5331), 1508-1510. https://doi.org/10.1126/science.277.5331.1508