© 2001 by Oxford University Press
Journal of the National Cancer Institute, Vol. 93, No. 19, 1449-1457,
October 3, 2001
© 2001 Oxford University Press
REVIEW |
Selective Estrogen Receptor Modulation and Reduction in Risk of Breast Cancer, Osteoporosis, and Coronary Heart Disease
Affiliations of authors: V. C. Jordan (Robert H. Lurie Comprehensive Cancer Center), S. Gapstur (Department of Preventive Medicine), M. Morrow (Department of Surgery), Northwestern University Medical School, Chicago, IL.
Correspondence to: V. Craig Jordan, Ph.D., D.Sc., Robert H. Lurie Comprehensive Cancer Center, 710 North Fairbanks Court, Olson Pavilion 8258, Chicago, IL 60611 (e-mail: vcjordan{at}nwu.edu).
The recognition of selective estrogen receptor modulation in the laboratory has resulted in the development of two selective estrogen receptor modulators (SERMs), tamoxifen and raloxifene, for clinical application in healthy women. SERMs are antiestrogenic in the breast but estrogen-like in the bones and reduce circulating cholesterol levels. SERMs also have different degrees of estrogenicity in the uterus. Tamoxifen is used specifically to reduce the incidence of breast cancer in premenopausal and postmenopausal women at risk for the disease. In contrast, raloxifene is used specifically to reduce the risk of osteoporosis in postmenopausal women at high risk for osteoporosis. The study of tamoxifen and raloxifene (STAR) trial is currently comparing the ability of these SERMs to reduce breast cancer incidence in high-risk postmenopausal women. There is intense interest in understanding the molecular mechanism(s) of action of SERMs at target sites in a woman's body. An understanding of the targeted actions of this novel drug group will potentially result in the introduction of new multifunctional medicines with applications as preventive agents or treatments of breast cancer and endometrial cancer, coronary heart disease, and osteoporosis.
This article has been cited by other articles:
![]() |
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] |
||||
![]() |
V. C. Jordan SERMs: Meeting the Promise of Multifunctional Medicines J Natl Cancer Inst, March 7, 2007; 99(5): 350 - 356. [Abstract] [Full Text] [PDF] |
||||
![]() |
R. T Chatterton Jr, J. Zujewski, E. T Mateo, J. Eng-Wong, and V C. Jordan Effect of raloxifene on salivary sex steroid concentrations in premenopausal women J. Endocrinol., December 1, 2006; 191(3): 599 - 604. [Abstract] [Full Text] [PDF] |
||||
![]() |
Y. Ogura, M. Azuma, Y. Tsuboi, Y. Kabe, Y. Yamaguchi, T. Wada, H. Watanabe, and H. Handa TFII-I down-regulates a subset of estrogen-responsive genes through its interaction with an initiator element and estrogen receptor {alpha} Genes Cells, April 1, 2006; 11(4): 373 - 381. [Abstract] [Full Text] [PDF] |
||||
![]() |
S. C.J.P. Gielen, C. W. Burger, L. C.M. Kuhne, P. Hanifi-Moghaddam, and L. J. Blok 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 Reproductive Sciences, October 1, 2005; 12(7): e55 - e66. [Abstract] [PDF] |
||||
![]() |
V. C. Jordan Chemoprevention in the 21st Century: Is a Balance Best or Should Women Have No Estrogen at All? J. Clin. Oncol., March 10, 2005; 23(8): 1598 - 1600. [Full Text] [PDF] |
||||
![]() |
U. Chatterji, J. E. Riby, T. Taniguchi, E. L. Bjeldanes, L. F. Bjeldanes, and G. L. Firestone Indole-3-carbinol stimulates transcription of the interferon gamma receptor 1 gene and augments interferon responsiveness in human breast cancer cells Carcinogenesis, July 1, 2004; 25(7): 1119 - 1128. [Abstract] [Full Text] [PDF] |
||||
![]() |
S. T. Pearce, H. Liu, I. Radhakrishnan, M. Abdelrahim, S. Safe, and V. C. Jordan Interaction of the Aryl Hydrocarbon Receptor Ligand 6-Methyl-1,3,8-trichlorodibenzofuran with Estrogen Receptor {alpha} Cancer Res., April 15, 2004; 64(8): 2889 - 2897. [Abstract] [Full Text] [PDF] |
||||
![]() |
S. Tang, H. Han, and V. B. Bajic ERGDB: Estrogen Responsive Genes Database Nucleic Acids Res., January 1, 2004; 32(90001): D533 - 536. [Abstract] [Full Text] [PDF] |
||||
![]() |
H. Liu, E.-S. Lee, C. Gajdos, S. T. Pearce, B. Chen, C. Osipo, J. Loweth, K. McKian, A. De Los Reyes, L. Wing, et al. Apoptotic Action of 17{beta}-Estradiol in Raloxifene-Resistant MCF-7 Cells In Vitro and In Vivo J Natl Cancer Inst, November 5, 2003; 95(21): 1586 - 1597. [Abstract] [Full Text] [PDF] |
||||
![]() |
T. Fujita, Y. Kobayashi, O. Wada, Y. Tateishi, L. Kitada, Y. Yamamoto, H. Takashima, A. Murayama, T. Yano, T. Baba, et al. Full Activation of Estrogen Receptor {alpha} Activation Function-1 Induces Proliferation of Breast Cancer Cells J. Biol. Chem., July 11, 2003; 278(29): 26704 - 26714. [Abstract] [Full Text] [PDF] |
||||
![]() |
B. H. Arjmandi, D. A. Khalil, B. J. Smith, E. A. Lucas, S. Juma, M. E. Payton, and R. A. Wild Soy Protein Has a Greater Effect on Bone in Postmenopausal Women Not on Hormone Replacement Therapy, as Evidenced by Reducing Bone Resorption and Urinary Calcium Excretion J. Clin. Endocrinol. Metab., March 1, 2003; 88(3): 1048 - 1054. [Abstract] [Full Text] [PDF] |
||||
![]() |
P. Webb, P. Nguyen, and P. J. Kushner Differential SERM Effects on Corepressor Binding Dictate ERalpha Activity in Vivo J. Biol. Chem., February 21, 2003; 278(9): 6912 - 6920. [Abstract] [Full Text] [PDF] |
||||
![]() |
J. D. Wulfkuhle, D. C. Sgroi, H. Krutzsch, K. McLean, K. McGarvey, M. Knowlton, S. Chen, H. Shu, A. Sahin, R. Kurek, et al. Proteomics of Human Breast Ductal Carcinoma in Situ Cancer Res., November 15, 2002; 62(22): 6740 - 6749. [Abstract] [Full Text] [PDF] |
||||
![]() |
D. Rivenzon-Segal, R. Margalit, and H. Degani Glycolysis as a metabolic marker in orthotopic breast cancer, monitored by in vivo 13C MRS Am J Physiol Endocrinol Metab, October 1, 2002; 283(4): E623 - E630. [Abstract] [Full Text] [PDF] |
||||
![]() |
D. A. Khalil, E. A. Lucas, S. Juma, B. J. Smith, M. E. Payton, and B. H. Arjmandi Soy Protein Supplementation Increases Serum Insulin-Like Growth Factor-I in Young and Old Men but Does Not Affect Markers of Bone Metabolism J. Nutr., September 1, 2002; 132(9): 2605 - 2608. [Abstract] [Full Text] [PDF] |
||||
![]() |
V. C. Jordan, H. Liu, and R. Dardes Re: Effect of Long-Term Estrogen Deprivation on Apoptotic Responses of Breast Cancer Cells to 17{beta}-Estradiol and The Two Faces of Janus: Sex Steroids as Mediators of Both Cell Proliferation and Cell Death J Natl Cancer Inst, August 7, 2002; 94(15): 1173 - 1173. [Full Text] [PDF] |
||||
![]() |
E. P. Winer, C. Hudis, H. J. Burstein, R. T. Chlebowski, J. N. Ingle, S. B. Edge, E. P. Mamounas, J. Gralow, L. J. Goldstein, K. I. Pritchard, et al. American Society of Clinical Oncology Technology Assessment on the Use of Aromatase Inhibitors as Adjuvant Therapy for Women With Hormone Receptor-Positive Breast Cancer: Status Report 2002 J. Clin. Oncol., August 1, 2002; 20(15): 3317 - 3327. [Abstract] [Full Text] [PDF] |
||||
![]() |
D. C. Kemp, P. W. Fan, and J. C. Stevens Characterization of Raloxifene Glucuronidation in Vitro: Contribution of Intestinal Metabolism to Presystemic Clearance Drug Metab. Dispos., June 1, 2002; 30(6): 694 - 700. [Abstract] [Full Text] [PDF] |
||||
![]() |
Y. Shang and M. Brown Molecular Determinants for the Tissue Specificity of SERMs Science, March 29, 2002; 295(5564): 2465 - 2468. [Abstract] [Full Text] [PDF] |
||||














