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Science 29 March 2002:
Vol. 295. no. 5564, pp. 2465 - 2468
DOI: 10.1126/science.1068537
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Reports

Molecular Determinants for the Tissue Specificity of SERMs

Yongfeng Shang, Myles Brown*

Selective estrogen receptor modulators (SERMs) mimic estrogen action in certain tissues while opposing it in others. The therapeutic effectiveness of SERMs such as tamoxifen and raloxifene in breast cancer depends on their antiestrogenic activity. In the uterus, however, tamoxifen is estrogenic. Here, we show that both tamoxifen and raloxifene induce the recruitment of corepressors to target gene promoters in mammary cells. In endometrial cells, tamoxifen, but not raloxifene, acts like estrogen by stimulating the recruitment of coactivators to a subset of genes. The estrogen-like activity of tamoxifen in the uterus requires a high level of steroid receptor coactivator 1 (SRC-1) expression. Thus cell type- and promoter-specific differences in coregulator recruitment determine the cellular response to SERMs.

Department of Adult Oncology, Dana-Farber Cancer Institute, 44 Binney Street, and Department of Medicine, Brigham and Women's Hospital and Harvard Medical School, Boston, MA 02115, USA.
*   To whom correspondence should be addressed. E-mail: myles_brown{at}dfci.harvard.edu

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A Novel Principle for Partial Agonism of Liver X Receptor Ligands: COMPETITIVE RECRUITMENT OF ACTIVATORS AND REPRESSORS.
M. Albers, B. Blume, T. Schlueter, M. B. Wright, I. Kober, C. Kremoser, U. Deuschle, and M. Koegl (2006)
J. Biol. Chem. 281, 4920-4930
   Abstract »    Full Text »    PDF »
Steroid Receptor Coactivator (SRC)-1 and SRC-3 Differentially Modulate Tissue-Specific Activation Functions of the Progesterone Receptor.
S. J. Han, F. J. DeMayo, J. Xu, S. Y. Tsai, M.-J. Tsai, and B. W. O'Malley (2006)
Mol. Endocrinol. 20, 45-55
   Abstract »    Full Text »    PDF »
Overexpression of the Coactivator Bridge-1 Results in Insulin Deficiency and Diabetes.
J. L. Volinic, J. H. Lee, K. Eto, V. Kaur, and M. K. Thomas (2006)
Mol. Endocrinol. 20, 167-182
   Abstract »    Full Text »    PDF »
Inhibition of estradiol-induced mammary proliferation by dibenzoylmethane through the E2-ER-ERE-dependent pathway.
C.-C. Lin, Y.-L. Tsai, M.-T. Huang, Y.-P. Lu, C.-T. Ho, S.-F. Tseng, and S.-C. Teng (2006)
Carcinogenesis 27, 131-136
   Abstract »    Full Text »    PDF »
Tamoxifen treatment for breast cancer enforces a distinct gene-expression profile on the human endometrium: an exploratory study.
S C J P Gielen, L C M Kuhne, P C Ewing, L J Blok, and C W Burger (2005)
Endocr. Relat. Cancer 12, 1037-1049
   Abstract »    Full Text »    PDF »
Recruitment of Histone Deacetylase 4 to the N-Terminal Region of Estrogen Receptor {alpha}.
H. Leong, J. R. Sloan, P. D. Nash, and G. L. Greene (2005)
Mol. Endocrinol. 19, 2930-2942
   Abstract »    Full Text »    PDF »
Interactions with p300 enhance transcriptional activation by the PDZ-domain coactivator Bridge-1.
J. H Lee, J. L Volinic, C. Banz, K.-M. Yao, and M. K Thomas (2005)
J. Endocrinol. 187, 283-292
   Abstract »    Full Text »    PDF »
Biology of Progesterone Receptor Loss in Breast Cancer and Its Implications for Endocrine Therapy.
X. Cui, R. Schiff, G. Arpino, C. K. Osborne, and A. V. Lee (2005)
J. Clin. Oncol. 23, 7721-7735
   Abstract »    Full Text »    PDF »
Analysis off Estrogen Agonism and Antagonism of Tamoxifen, Raloxifene, and ICI182780 in Endometrial Cancer Cells: A Putative Role for the Epidermal Growth Factor Receptor Ligand Amphiregulin.
S. C.J.P. Gielen, C. W. Burger, L. C.M. Kuhne, P. Hanifi-Moghaddam, and L. J. Blok (2005)
Reproductive Sciences 12, e55-e66
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Androgen Dependent Mammary Gland Virilism in Rats Given the Selective Estrogen Receptor Modulator LY2066948 Hydrochloride.
D. G. Rudmann, I. R. Cohen, M. R. Robbins, D. E. Coutant, and J. W. Henck (2005)
Toxicol Pathol 33, 711-719
   Abstract »    Full Text »    PDF »
Modulator Recognition Factor 1, an AT-Rich Interaction Domain Family Member, Is a Novel Corepressor for Estrogen Receptor {alpha}.
S. P. Georgescu, J. H. Li, Q. Lu, R. H. Karas, M. Brown, and M. E. Mendelsohn (2005)
Mol. Endocrinol. 19, 2491-2501
   Abstract »    Full Text »    PDF »
The p160 family coactivators regulate breast cancer cell proliferation and invasion through autocrine/paracrine activity of SDF-1{alpha}/CXCL12.
H. Kishimoto, Z. Wang, P. Bhat-Nakshatri, D. Chang, R. Clarke, and H. Nakshatri (2005)
Carcinogenesis 26, 1706-1715
   Abstract »    Full Text »    PDF »
Trastuzumab Therapy for Tamoxifen-Stimulated Endometrial Cancer.
C. Osipo, K. Meeke, H. Liu, D. Cheng, S. Lim, A. Weichel, and V. C. Jordan (2005)
Cancer Res. 65, 8504-8513
   Abstract »    Full Text »    PDF »
Estrogen down-regulation of the corepressor N-CoR: Mechanism and implications for estrogen derepression of N-CoR-regulated genes.
J. Frasor, J. M. Danes, C. C. Funk, and B. S. Katzenellenbogen (2005)
PNAS 102, 13153-13157
   Abstract »    Full Text »    PDF »
Peptide Binding Identifies an ER{alpha} Conformation That Generates Selective Activity in Multiple In Vitro Assays.
C. J. Larson, D. L. Osburn, K. Schmitz, L. Giampa, S.-M. Mong, K. Marschke, H. M. Seidel, J. Rosen, and A. Negro-Vilar (2005)
J Biomol Screen 10, 590-598
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Bazedoxifene Acetate: A Selective Estrogen Receptor Modulator with Improved Selectivity.
B. S. Komm, Y. P. Kharode, P. V. N. Bodine, H. A. Harris, C. P. Miller, and C. R. Lyttle (2005)
Endocrinology 146, 3999-4008
   Abstract »    Full Text »    PDF »
Glucocorticoid Receptor Point Mutation V571M Facilitates Coactivator and Ligand Binding by Structural Rearrangement and Stabilization.
P. Carlsson, K. F. Koehler, and L. Nilsson (2005)
Mol. Endocrinol. 19, 1960-1977
   Abstract »    Full Text »    PDF »


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