![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
Vol. 295, Issue 2, 431-437, November 2000
Department of Molecular and Cellular Biology, Baylor College of
Medicine, Houston, Texas
In females, estrogens play a key role in reproduction and have
beneficial effects on the skeletal, cardiovascular, and central nervous
systems. Most estrogenic responses are mediated by estrogen receptors
(ERs), either ER
or ER
, which are members of the nuclear receptor
superfamily of ligand-dependent transcription factors. Selective
estrogen receptor modulators (SERMs) are ER ligands that in some
tissues act like estrogens, but block estrogen action in others. Thus,
SERMs may exhibit an agonistic or antagonistic biocharacter depending
on the context in which their activity is examined. For example, the
SERMs tamoxifen and raloxifene both exhibit ER antagonist activity in
breast and agonist activity in bone, but only tamoxifen manifests
agonist activity in the uterus. Numerous studies have examined the
molecular basis for SERM selectivity. Collectively they indicate that
different ER ligands induce distinct structural changes in the receptor
that influence its ability to interact with other proteins (e.g.,
coactivators or corepressors) critical for the regulation of target
gene transcription. The relative expression of coactivators and
corepressors, and the nature of the ER and of its target gene promoter
affect SERM biocharacter. Taken together, SERM selectivity reflects the
diversity of ER forms and coregulators, cell type differences in their
expression, and the diversity of ER target genes. This model provides a
basis for understanding the molecular mechanisms of SERM action, and should help identify new SERMs with enhanced tissue or target gene selectivity.
This article has been cited by other articles:
|
|
 |
|
  G. Orasanu, O. Ziouzenkova, P. R. Devchand, V. Nehra, O. Hamdy, E. S. Horton, and J. Plutzky The Peroxisome Proliferator-Activated Receptor-{gamma} Agonist Pioglitazone Represses Inflammation in a Peroxisome Proliferator-Activated Receptor-{alpha}-Dependent Manner In Vitro and In Vivo in Mice J. Am. Coll. Cardiol., September 2, 2008; 52(10): 869 - 881. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. M. Wilkinson, S. Hayes, D. Thompson, P. Whitney, and K. Bi Compound Profiling Using a Panel of Steroid Hormone Receptor Cell-Based Assays J Biomol Screen, September 1, 2008; 13(8): 755 - 765. [Abstract] [PDF]
|
|
|
|
 |
|
 E. Carreras, S. Turner, V. Paharkova-Vatchkova, A. Mao, C. Dascher, and S. Kovats Estradiol Acts Directly on Bone Marrow Myeloid Progenitors to Differentially Regulate GM-CSF or Flt3 Ligand-Mediated Dendritic Cell Differentiation J. Immunol., January 15, 2008; 180(2): 727 - 738. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 L. Bertelsen, L. Bernstein, J. H. Olsen, L. Mellemkjaer, R. W. Haile, C. F. Lynch, K. E. Malone, H. Anton-Culver, J. Christensen, B. Langholz, et al. Effect of Systemic Adjuvant Treatment on Risk for Contralateral Breast Cancer in the Women's Environment, Cancer and Radiation Epidemiology Study J Natl Cancer Inst, January 2, 2008; 100(1): 32 - 40. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 A. D. Benninghoff and D. E. Williams Identification of a Transcriptional Fingerprint of Estrogen Exposure in Rainbow Trout Liver Toxicol. Sci., January 1, 2008; 101(1): 65 - 80. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. Bartsch, C. Wenzel, G. Altorjai, U. Pluschnig, R. M. Mader, M. Gnant, R. Jakesz, M. Rudas, C. C. Zielinski, and G. G. Steger Her2 and Progesterone Receptor Status Are Not Predictive of Response to Fulvestrant Treatment Clin. Cancer Res., August 1, 2007; 13(15): 4435 - 4439. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 L. Li, M. E Andersen, S. Heber, and Q. Zhang Non-monotonic dose-response relationship in steroid hormone receptor-mediated gene expression J. Mol. Endocrinol., May 1, 2007; 38(5): 569 - 585. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J. Ostrowski, J. E. Kuhns, J. A. Lupisella, M. C. Manfredi, B. C. Beehler, S. R. Krystek Jr., Y. Bi, C. Sun, R. Seethala, R. Golla, et al. Pharmacological and X-Ray Structural Characterization of a Novel Selective Androgen Receptor Modulator: Potent Hyperanabolic Stimulation of Skeletal Muscle with Hypostimulation of Prostate in Rats Endocrinology, January 1, 2007; 148(1): 4 - 12. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
A. Mao, V. Paharkova-Vatchkova, J. Hardy, M. M. Miller, and S. Kovats Estrogen Selectively Promotes the Differentiation of Dendritic Cells with Characteristics of Langerhans Cells J. Immunol., October 15, 2005; 175(8): 5146 - 5151. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
G. Nalbandian, V. Paharkova-Vatchkova, A. Mao, S. Nale, and S. Kovats The Selective Estrogen Receptor Modulators, Tamoxifen and Raloxifene, Impair Dendritic Cell Differentiation and Activation J. Immunol., August 15, 2005; 175(4): 2666 - 2675. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
E. Peeva, J. Venkatesh, and B. Diamond Tamoxifen Blocks Estrogen-Induced B Cell Maturation but Not Survival J. Immunol., August 1, 2005; 175(3): 1415 - 1423. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 Y. M. Shah, M. Al-Dhaheri, Y. Dong, C. Ip, F. E. Jones, and B. G. Rowan Selenium disrupts estrogen receptor {alpha} signaling and potentiates tamoxifen antagonism in endometrial cancer cells and tamoxifen-resistant breast cancer cells Mol. Cancer Ther., August 1, 2005; 4(8): 1239 - 1249. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. Zhang, T. McElrath, W. Tong, and J. W Pollard The molecular basis of tamoxifen induction of mouse uterine epithelial cell proliferation J. Endocrinol., January 1, 2005; 184(1): 129 - 140. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 R. Soares, G. Balogh, S. Guo, F. Gartner, J. Russo, and F. Schmitt Evidence for the Notch Signaling Pathway on the Role of Estrogen in Angiogenesis Mol. Endocrinol., September 1, 2004; 18(9): 2333 - 2343. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
V. Paharkova-Vatchkova, R. Maldonado, and S. Kovats Estrogen Preferentially Promotes the Differentiation of CD11c+ CD11bintermediate Dendritic Cells from Bone Marrow Precursors J. Immunol., February 1, 2004; 172(3): 1426 - 1436. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 H. Ogita, K. Node, Y. Liao, F. Ishikura, S. Beppu, H. Asanuma, S. Sanada, S. Takashima, T. Minamino, M. Hori, et al. Raloxifene Prevents Cardiac Hypertrophy and Dysfunction in Pressure-Overloaded Mice Hypertension, February 1, 2004; 43(2): 237 - 242. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. M. Rangwala and M. A. Lazar The Dawn of the SPPARMs? Sci. Signal., February 26, 2002; 2002(121): pe9 - pe9. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 K. Hisamoto, M. Ohmichi, Y. Kanda, K. Adachi, Y. Nishio, J. Hayakawa, S. Mabuchi, K. Takahashi, K. Tasaka, Y. Miyamoto, et al. Induction of Endothelial Nitric-oxide Synthase Phosphorylation by the Raloxifene Analog LY117018 Is Differentially Mediated by Akt and Extracellular Signal-regulated Protein Kinase in Vascular Endothelial Cells J. Biol. Chem., December 7, 2001; 276(50): 47642 - 47649. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 S. Signoretti and M. Loda Estrogen Receptor {beta} in Prostate Cancer : Brake Pedal or Accelerator? Am. J. Pathol., July 1, 2001; 159(1): 13 - 16. [Full Text] [PDF]
|
|
|
|
 |
|
 L. O'Donnell, K. M. Robertson, M. E. Jones, and E. R. Simpson Estrogen and Spermatogenesis Endocr. Rev., June 1, 2001; 22(3): 289 - 318. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
