Differential Ligand Activation of Estrogen Receptors ERα and ERβ at AP1 Sites-Reference-Cited by-同舟云学术

Differential Ligand Activation of Estrogen Receptors ERα and ERβ at AP1 Sites

Published:1997-09-05 Issue:5331 Volume:277 Page:1508-1510
ISSN:0036-8075
Container-title:Science
language:en
Short-container-title:Science

Author:

Paech Kolja¹²³⁴⁵,Webb Paul¹²³⁴⁵,Kuiper George G. J. M.¹²³⁴⁵,Nilsson Stefan¹²³⁴⁵,Gustafsson Jan-Åke¹²³⁴⁵,Kushner Peter J.¹²³⁴⁵,Scanlan Thomas S.¹²³⁴⁵

Affiliation:

1. K. Paech and T. S. Scanlan, Departments of Pharmaceutical Chemistry and Cellular and Molecular Pharmacology, University of California, San Francisco, CA 94143–0446, USA.

2. P. Webb and P. J. Kushner, Metabolic Research Unit, University of California, San Francisco, CA 94143–0540, USA.

3. G. G. J. M. Kuiper, Center for Biotechnology, Karolinska Institute, Novum, S-14186 Huddinge, Sweden.

4. S. Nilsson, Karo Bio AB, Novum, S-14157 Huddinge, Sweden.

5. J.-Å. Gustafsson, Center for Biotechnology and Department of Medical Nutrition, Karolinska Institute, Novum, S-14186 Huddinge, Sweden.

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.

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

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