Note to users. If you're seeing this message, it means that your browser cannot find this page's style/presentation instructions -- or possibly that you are using a browser that does not support current Web standards. Find out more about why this message is appearing, and what you can do to make your experience of our site the best it can be.
Also see the archival list of Science's Compass: Enhanced Perspectives
BIOMEDICINE: Enhanced: Defining the "S" in SERMs
Benita S. Katzenellenbogen and John A. Katzenellenbogen
Tamoxifen, which opposes estrogen action in some tissues while mimicking its action in others, has reduced breast cancer mortality significantly during the past decade. In their Perspective, Katzenellenbogen and Katzenellenbogen discuss new findings (Shang and Brown) that unravel the molecular basis of tamoxifen's differential activity in breast and uterine tissue.
The authors are in the Department of Molecular and Integrative Physiology and the Department of Cell and Structural Biology, University of Illinois and College of Medicine at Urbana-Champaign, and in the Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801, USA. E-mail: katzenel{at}life.uiuc.edu
Estrogen Receptor (ER) {beta} Modulates ER{alpha} Responses to Estrogens in the Developing Rat Ventromedial Nucleus of the Hypothalamus.
K. L. Gonzales, M. J. Tetel, and C. K. Wagner (2008)
Endocrinology
149, 4615-4621
|Abstract »|Full Text »|PDF »
Coactivators PGC-1beta and SRC-1 Interact Functionally to Promote the Agonist Activity of the Selective Estrogen Receptor Modulator Tamoxifen.
D. Kressler, M. B. Hock, and A. Kralli (2007)
J. Biol. Chem.
282, 26897-26907
|Abstract »|Full Text »|PDF »
Estrogen-Regulated Gene Networks in Human Breast Cancer Cells: Involvement of E2F1 in the Regulation of Cell Proliferation.
J. D. Stender, J. Frasor, B. Komm, K. C. N. Chang, W. L. Kraus, and B. S. Katzenellenbogen (2007)
Mol. Endocrinol.
21, 2112-2123
|Abstract »|Full Text »|PDF »
Structural modulation of reactivity/activity in design of improved benzothiophene selective estrogen receptor modulators: induction of chemopreventive mechanisms.
B. Yu, B. M. Dietz, T. Dunlap, I. Kastrati, D. D. Lantvit, C. R. Overk, P. Yao, Z. Qin, J. L. Bolton, and G. R.J. Thatcher (2007)
Mol. Cancer Ther.
6, 2418-2428
|Abstract »|Full Text »|PDF »
Estrogen Receptors: How Do They Signal and What Are Their Targets.
N. Heldring, A. Pike, S. Andersson, J. Matthews, G. Cheng, J. Hartman, M. Tujague, A. Strom, E. Treuter, M. Warner, et al. (2007)
Physiol Rev
87, 905-931
|Abstract »|Full Text »|PDF »
Integration of Steroid and Growth Factor Pathways in Breast Cancer: Focus on Signal Transducers and Activators of Transcription and Their Potential Role in Resistance.
Structural Insights into Corepressor Recognition by Antagonist-bound Estrogen Receptors.
N. Heldring, T. Pawson, D. McDonnell, E. Treuter, J.-A. Gustafsson, and A. C. W. Pike (2007)
J. Biol. Chem.
282, 10449-10455
|Abstract »|Full Text »|PDF »
The Liver X Receptor (LXR) and Hepatic Lipogenesis: THE CARBOHYDRATE-RESPONSE ELEMENT-BINDING PROTEIN IS A TARGET GENE OF LXR.
Gene expression preferentially regulated by tamoxifen in breast cancer cells and correlations with clinical outcome..
J. Frasor, E. C. Chang, B. Komm, C.-Y. Lin, V. B. Vega, E. T. Liu, L. D. Miller, J. Smeds, J. Bergh, and B. S. Katzenellenbogen (2006)
Cancer Res.
66, 7334-7340
|Abstract »|Full Text »|PDF »
Estrogen-occupied Estrogen Receptor Represses Cyclin G2 Gene Expression and Recruits a Repressor Complex at the Cyclin G2 Promoter.
F. Stossi, V. S. Likhite, J. A. Katzenellenbogen, and B. S. Katzenellenbogen (2006)
J. Biol. Chem.
281, 16272-16278
|Abstract »|Full Text »|PDF »
Coregulators in Nuclear Estrogen Receptor Action: From Concept to Therapeutic Targeting.
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 »
The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers.
K-M Rau, H-Y Kang, T-L Cha, S A Miller, and M-C Hung (2005)
Endocr. Relat. Cancer
12, 511-532
|Abstract »|Full Text »|PDF »
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 »
Estrogen Receptor {alpha} and {beta} Heterodimers Exert Unique Effects on Estrogen- and Tamoxifen-Dependent Gene Expression in Human U2OS Osteosarcoma Cells.
D. G. Monroe, F. J. Secreto, M. Subramaniam, B. J. Getz, S. Khosla, and T. C. Spelsberg (2005)
Mol. Endocrinol.
19, 1555-1568
|Abstract »|Full Text »|PDF »
Anti-proliferative effect of estrogen in breast cancer cells that re-express ER{alpha} is mediated by aberrant regulation of cell cycle genes.
J G Moggs, T C Murphy, F L Lim, D J Moore, R Stuckey, K Antrobus, I Kimber, and G Orphanides (2005)
J. Mol. Endocrinol.
34, 535-551
|Abstract »|Full Text »|PDF »
Delineation of a unique protein-protein interaction site on the surface of the estrogen receptor.
E. H. Kong, N. Heldring, J.-A. Gustafsson, E. Treuter, R. E. Hubbard, and A. C. W. Pike (2005)
PNAS
102, 3593-3598
|Abstract »|Full Text »|PDF »
Distinct gene expression patterns in a tamoxifen-sensitive human mammary carcinoma xenograft and its tamoxifen-resistant subline MaCa 3366/TAM.
M. Becker, A. Sommer, J. R. Kratzschmar, H. Seidel, H.-D. Pohlenz, and I. Fichtner (2005)
Mol. Cancer Ther.
4, 151-170
|Abstract »|Full Text »|PDF »
Arzoxifene: A Promising New Selective Estrogen Receptor Modulator for Clinical Chemoprevention of Breast Cancer: Commentary re C. J. Fabian et al., Breast Cancer Chemoprevention Phase I Evaluation of Biomarker Modulation by Arzoxifene, a Third Generation Selective Estrogen Receptor Modulator. Clin Cancer Res 2004;10:5403-17..
M. B. Sporn (2004)
Clin. Cancer Res.
10, 5313-5315
|Full Text »|PDF »
Transcriptional Profiling of Estrogen-Regulated Gene Expression via Estrogen Receptor (ER) {alpha} or ER{beta} in Human Osteosarcoma Cells: Distinct and Common Target Genes for These Receptors.
F. Stossi, D. H. Barnett, J. Frasor, B. Komm, C. R. Lyttle, and B. S. Katzenellenbogen (2004)
Endocrinology
145, 3473-3486
|Abstract »|Full Text »|PDF »
Identification of Tamoxifen-Induced Coregulator Interaction Surfaces within the Ligand-Binding Domain of Estrogen Receptors.
N. Heldring, M. Nilsson, B. Buehrer, E. Treuter, and J.-A. Gustafsson (2004)
Mol. Cell. Biol.
24, 3445-3459
|Abstract »|Full Text »|PDF »
Recruitment of Distinct Chromatin-modifying Complexes by Tamoxifen-complexed Estrogen Receptor at Natural Target Gene Promoters in Vivo.
Selective Estrogen Receptor Modulators: Discrimination of Agonistic versus Antagonistic Activities by Gene Expression Profiling in Breast Cancer Cells.
J. Frasor, F. Stossi, J. M. Danes, B. Komm, C. R. Lyttle, and B. S. Katzenellenbogen (2004)
Cancer Res.
64, 1522-1533
|Abstract »|Full Text »|PDF »
Profiling of Estrogen Up- and Down-Regulated Gene Expression in Human Breast Cancer Cells: Insights into Gene Networks and Pathways Underlying Estrogenic Control of Proliferation and Cell Phenotype.
J. Frasor, J. M. Danes, B. Komm, K. C. N. Chang, C. R. Lyttle, and B. S. Katzenellenbogen (2003)
Endocrinology
144, 4562-4574
|Abstract »|Full Text »|PDF »
The Interplay between the Glucocorticoid Receptor and Nuclear Factor-{kappa}B or Activator Protein-1: Molecular Mechanisms for Gene Repression.
K. De Bosscher, W. Vanden Berghe, and G. Haegeman (2003)
Endocr. Rev.
24, 488-522
|Abstract »|Full Text »|PDF »
Response-Specific and Ligand Dose-Dependent Modulation of Estrogen Receptor (ER) {alpha} Activity by ER{beta} in the Uterus.
J. Frasor, D. H. Barnett, J. M. Danes, R. Hess, A. F. Parlow, and B. S. Katzenellenbogen (2003)
Endocrinology
144, 3159-3166
|Abstract »|Full Text »|PDF »
Control of Follicle-Stimulating Hormone by Estradiol and the Inhibins: Critical Role of Estradiol at the Hypothalamus during the Luteal-Follicular Transition.
C. K. Welt, Y. L. Pagan, P. C. Smith, K. B. Rado, and J. E. Hall (2003)
J. Clin. Endocrinol. Metab.
88, 1766-1771
|Abstract »|Full Text »|PDF »
Regulation of Nuclear Receptor Transcriptional Activity by a Novel DEAD Box RNA Helicase (DP97).
R. R. Rajendran, A. C. Nye, J. Frasor, R. D. Balsara, P. G. V. Martini, and B. S. Katzenellenbogen (2003)
J. Biol. Chem.
278, 4628-4638
|Abstract »|Full Text »|PDF »
Mechanism of Action of Progesterone Antagonists.
S. A. Leonhardt and D. P. Edwards (2002)
Experimental Biology and Medicine
227, 969-980
|Abstract »|Full Text »
Raloxifene, a Mixed Estrogen Agonist/Antagonist, Induces Apoptosis in Androgen-independent Human Prostate Cancer Cell Lines.
I. Y. Kim, B.-C. Kim, D. H. Seong, D. K. Lee, J.-M. Seo, Y. J. Hong, H.-T. Kim, R. A. Morton, and S.-J. Kim (2002)
Cancer Res.
62, 5365-5369
|Abstract »|Full Text »|PDF »
