Distinct effects of the antiestrogen Faslodex on the stability of estrogen receptors-alpha and -beta in the breast cancer cell line MCF-7

Peekhaus, N.T.; Chang, T.; Hayes, E.C.; Wilkinson, H.A.; Mitra, S.W.; Schaeffer, J.M.; Rohrer, S.P.

Journal of Molecular Endocrinology 32(3): 987-995


ISSN/ISBN: 0952-5041
PMID: 15171727
DOI: 10.1677/jme.0.0320987
Accession: 011967387

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The effects of estrogen receptor (ER) ligands on the stability and transcriptional activity of ERbeta in the breast cancer cell lines MCF-7 and HeLa were examined. We found that ERbeta was degraded in the presence of 17beta-estradiol. Tamoxifen and Faslodex (ICI 182,780) prevented ERbeta receptor destabilization. In contrast to ERalpha, ERbeta degradation was not abolished by inhibitors of the proteasome-mediated protein degradation pathway. Furthermore, single point mutations in helix 12 of the receptor dramatically affected the stability and subsequent transcriptional activation of ERbeta.