Selective Estrogen Receptor Modulation: The Search for an Ideal Hormonal Therapy for Breast Cancer

REFERENCES

• Hulka B. S. Epidemiology of Susceptibility to Breast Cancer. Prog. Clin. Biol. Res. 1996; 395: 159–174
   PubMedGoogle Scholar
• Guillino P. M., Pettigrew H. M., Grantham F. H. N-Nitrosomethylurea as a Mammary Gland Carcinogen in Rats. J. Natl. Cancer Inst. 1975; 54: 401–414
   PubMed Web of Science ®Google Scholar
• Jaiyesimi I. A., Buzdar A. U., Decker D. A., et al. Use of Tamoxifen for Breast Cancer: Twenty-Eight Years Later. J. Clin. Oncol. 1995; 13: 513–529
   PubMed Web of Science ®Google Scholar
• Hayes D. F., Van Zyl J. A., Hacking A., et al. Randomized Comparison of Tamoxifen and Two Separate Doses of Toremifene in Postmenopausal Patients with Metastatic Breast Cancer. J. Clin. Oncol. 1995; 13: 2556–2566
   PubMed Web of Science ®Google Scholar
• Gershanovich M., Garin A., Baltina D., et al. A Phase III Comparison of Two Toremiphene Doses to Tamoxifen in Postmenopausal Women with Advanced Breast Cancer. Breast Cancer Res. Treat 1997; 45: 251–262
   PubMed Web of Science ®Google Scholar
• Gale K. E., Andersen J. W., Tormey D. C., et al. Hormonal Treatment for Metastatic Breast Cancer: An Eastern Cooperative Oncology Group Phase III Trial Comparing Aminoglutethimide to Tamoxifen. Cancer 1994; 73: 354–361
   PubMed Web of Science ®Google Scholar
• Early Breast Cancer Trialists' Collaborative Group: Tamoxifen for Early Breast Cancer: An Overview of the Randomised Trials. Lancet 1998; 351: 1451–1467
   PubMed Web of Science ®Google Scholar
• Fisher B., Constantino J. P., Wickerham D. L., et al. Tamoxifen for Prevention of Breast Cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study. J. Natl. Cancer Inst. 1998; 90: 1371–1388
   PubMed Web of Science ®Google Scholar
• Veronesi U., Maisonneuve P., Costa A., et al. Prevention of Breast Cancer with Tamoxifen: Preliminary Findings from the Italian Randomised Trial Among Hysterectomized Women. Lancet 1998; 352: 93–97
   PubMed Web of Science ®Google Scholar
• Powles T., Eeles R., Ashley S., et al. Interim Analysis of the Incidence of Breast Cancer in the Royal Marsden Hospital Tamoxifen Randomised Chemoprevention Trial. Lancet 1998; 352: 98–101
   PubMed Web of Science ®Google Scholar
• Pritchard K. I. Is Tamoxifen Effective in Prevention of Breast Cancer?. Lancet 1998; 352: 80–81
   PubMed Web of Science ®Google Scholar
• Powles T. J., Hickish T., Kanis J. A., et al. Effect of Tamoxifen on Bone Mineral Density Measured by Dual-Energy X-ray Absorptiometry in Healthy Premenopausal and Postmenopausal Women. J. Clin. Oncol. 1996; 14: 78–84
   PubMed Web of Science ®Google Scholar
• Costantino J. P., Kuller L. H., Ives D. G., et al. Coronary Heart Disease Mortality and Adjuvant Tamoxifen Therapy. J. Natl. Cancer Inst. 1997; 89: 776–782
   PubMed Web of Science ®Google Scholar
• Rutqvist L. E., Mattsson A. Cardiac and Thromboembolic Morbidity Among Postmenopausal Women with Early-Stage Breast Cancer in a Randomized Trial of Adjuvant Tamoxifen. J. Natl. Cancer Inst. 1993; 85: 1398–1406
   PubMed Web of Science ®Google Scholar
• Fisher B., Costantino J. P., Redmond C. K., et al. Endometrial Cancer in Tamoxifen-Treated Breast Cancer Patients: Findings from the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14. J. Natl. Cancer Inst. 1994; 86: 527–537
   PubMed Web of Science ®Google Scholar
• Hann L. E., Giess C. S., Bach A. M., et al. Endometrial Thickness in Tamoxifen-Treated Patients: Correlation with Clinical and Pathologic Findings. Am. J. Roentgenol. 1997; 168: 657–661
   PubMed Web of Science ®Google Scholar
• Marconi D., Exacoustos C., Cangi B., et al. Transvaginal Sonographic and Hysteroscopic Findings in Postmenopausal Women Receiving Tamoxifen. J. Am. Assoc. Gynecol. Laparoscopists 1997; 4: 331–339
   PubMedGoogle Scholar
• Bertelli G., Cosso M., Cusimano E., et al. Tamoxifen and the Endometrium: Findings of Pelvic Ultrasound Examination and Endometrial Biopsy in Asymptomatic Breast Cancer Patients. Breast Cancer Res. Treat 1998; 47: 41–46
   PubMed Web of Science ®Google Scholar
• Kedar R. P., Bourne T. H., Powles T. J., et al. Effects of Tamoxifen on Uterus and Ovaries of Postmenopausal Women in a Randomised Breast Cancer Prevention Trial. Lancet 1994; 343: 1318–1321
   PubMed Web of Science ®Google Scholar
• Fornander T., Rutqvist L. E., Cedermark B., et al. Adjuvant Tamoxifen in Early-Stage Breast Cancer: Effects on Intercurrent Morbidity and Mortality. J. Clin. Oncol. 1991; 9: 1740–1748
   PubMed Web of Science ®Google Scholar
• Nayfield S. G., Gorin M. B. Tamoxifen-Associated Eye Disease: A Review. J. Clin. Oncol. 1996; 14: 1018–1026
   PubMed Web of Science ®Google Scholar
• Han X., Liehr J. G. Induction of Covalent DNA Adducts in Rodents by Tamoxifen. Cancer Res. 1992; 52: 1360–1363
   PubMed Web of Science ®Google Scholar
• Li D. H., Dragan Y., Jordan V. C., et al. Effects of Chronic Administration of Tamoxifen and Toremifene on DNA Adducts in Rat Liver, Kidney, and Uterus. Cancer Res. 1997; 57: 1438–1441
   PubMed Web of Science ®Google Scholar
• Hemminki K., Rajaniemi H., Lindahl B., et al. Tamoxifen-Induced DNA Adducts in Endometrial Samples from Breast Cancer Patients. Cancer Res. 1996; 56: 4374–4377
   PubMed Web of Science ®Google Scholar
• Johnston S. R.D., Saccani-Jotti G., Smith I. E., et al. Changes in Estrogen Receptor, Progesterone Receptor, and pS2 Expression in Tamoxifen-Resistant Human Breast Cancer. Cancer Res. 1995; 55: 3331–3338
   PubMed Web of Science ®Google Scholar
• Johnston S. R.D., Lu B., Dowsett M., et al. Comparison of Estrogen Receptor DNA Binding in Untreated and Acquired Antiestrogen-Resistant Human Breast Tumors. Cancer Res. 1997; 57: 3723–3727
   PubMed Web of Science ®Google Scholar
• Leygue E., Huang A. H., Murphy L. C., et al. Prevalence of Estrogen Receptor Variant Messenger RNAs in Human Breast Cancer. Cancer Res. 1996; 56: 4324–4327
   PubMed Web of Science ®Google Scholar
• Zhang Q. X., Hilsenbeck S. G., Fuqua S. A.W., et al. Multiple Splicing Variants of the Estrogen Receptor Are Present in Individual Human Breast Tumors. J. Steroid Biochem. Mol. Biol. 1996; 59: 251–260
   PubMed Web of Science ®Google Scholar
• Daffada A. A.I., Johnston S. R.D., Smith I. E., et al. Exon 5 Deletion Variant Estrogen Receptor Messenger RNA Expression in Relation to Tamoxifen Resistance and Progesterone Receptor/pS2 Status in Human Breast Cancer. Cancer Res. 1995; 55: 288–293
   PubMed Web of Science ®Google Scholar
• Gottardis M. M., Jordan V. C. Development of Tamoxifen-Stimulated Growth of MCF-7 Tumors in Athymic Mice After Long-Term Antiestrogen Administration. Cancer Res. 1988; 48: 5183–5187
   PubMed Web of Science ®Google Scholar
• Osborne C. K., Coronado E. B. Robinson, J.P. Human Breast Cancer in the Athymic Nude Mouse: Cytostatic Effects of Long-Term Antiestrogen Therapy. Eur. J. Cancer Clin. Oncol. 1987; 23: 1189–1196
   PubMedGoogle Scholar
• Fisher B., Dignam J., Bryant J., et al. Five Versus More Than Five Years of Tamoxifen Therapy for Breast Cancer Patients with Negative Lymph Nodes and Estrogen Receptor-Positive Tumors. J. Natl. Cancer Inst. 1996; 88: 1529–1542
   PubMed Web of Science ®Google Scholar
• Wiebe V. J., Osborne C. K., McGuire W. L., et al. Identification of Estrogenic Tamoxifen Metabolite(s) in Tamoxifen-Resistant Human Breast Tumors. J. Clin. Oncol. 1992; 10: 990–994
   PubMed Web of Science ®Google Scholar
• Wolf D. M., Langan-Fahey S. M., Parker C. J., et al. Investigation of the Mechanism of Tamoxifen-Stimulated Breast Tumor Growth with Nonisomerizable Analogues of Tamoxifen and Metabolites. J. Natl. Cancer Inst. 1993; 85: 806–812
   PubMed Web of Science ®Google Scholar
• Langan-Fahey S. M., Tormey D. C., Jordan V. C. Tamoxifen Metabolites in Patients on Long-Term Adjuvant Therapy for Breast Cancer. Eur. J. Cancer 1990; 26: 883–888
   PubMed Web of Science ®Google Scholar
• Dumont J. A., Bitoni A. J., Wallace C. D., et al. Progression of MCF-7 Breast Cancer Cells to Antiestrogen-Resistant Phenotype Is Accompanied by Elevated Levels of AP-1 DNA-Binding Activity. Cell Growth Differ. 1996; 7: 351–359
   PubMedGoogle Scholar
• Johnston S. R.D., Lu B., Scott G. K., et al. Increased Activator Protein-1 DNA Binding and c-Jun NH2-Terminal Kinase Activity in Human Breast Tumors with Acquired Tamoxifen Resistance. Clin. Cancer Res. 1999; 5: 251–256
   PubMed Web of Science ®Google Scholar
• Wiseman L. R., Johnson M. D., Wakeling A. E., et al. Type I IGF Receptor and Acquired Tamoxifen Resistance in Oestrogen-Responsive Human Breast Cancer Cells. Eur. J. Cancer 1993; 29A: 2256–2264
   PubMed Web of Science ®Google Scholar
• Van der Burg B., De Groot R. P., Isbrücker L., et al. Oestrogen Directly Stimulates Growth Factor Signal Transduction Pathways in Human Breast Cancer Cells. J. Steroid Biochem. Mol. Biol. 1991; 40: 215–221
   PubMed Web of Science ®Google Scholar
• Haarstad H., Lonning P. E., Gundersen S., et al. Influence of Droloxifene on Metastatic Breast Cancer as First-Line Endocrine Treatment. Acta Oncol. 1998; 37: 365–368
   PubMed Web of Science ®Google Scholar
• Marttunen M. B., Hietanen P., Tiitinen A., et al. Comparison of Effects of Tamoxifen and Toremifene on Bone Biochemistry and Bone Mineral Density in Postmenopausal Breast Cancer Patients. J. Clin. Endocrinol. Metab. 1998; 83: 1158–1162
   PubMed Web of Science ®Google Scholar
• Howell A., DeFriend D. J., Robertson J. F.R., et al. Pharmacokinetics, Pharmacological and Anti-Tumour Effects of the Specific Anti-Oestrogen ICI 182780 in Women with Advanced Breast Cancer. Br. J. Cancer 1996; 74: 300–308
   PubMed Web of Science ®Google Scholar
• Sibonga J. D., Dobnig H., Harden R. M., et al. Effect of the High-Affinity Estrogen Receptor Ligand ICI 182780 on the Rat Tibia. Endocrinology 1998; 139: 3736–3742
   PubMed Web of Science ®Google Scholar
• Delmas P. D., Bjarnson N. H., Mitlak B. H., et al. Effects of Raloxifene on Bone Mineral Density, Serum Cholesterol Concentrations, and Uterine Endometrium in Postmenopausal Women. N. Engl. J. Med. 1997; 337: 1641–1647
   PubMed Web of Science ®Google Scholar
• Ettinger B., Black D. M., Mitlak B. H., et al. Reduction of Vertebral Fracture Risk in Postmenopausal Women with Osteoporosis Treated with Raloxifene—Results from a 3-Year Randomized Clinical Trial. JAMA 1999; 282: 637–645
   PubMed Web of Science ®Google Scholar
• Cummings S. R., Eckert S., Krueger K. A., et al. The Effect of Raloxifene on Risk of Breast Cancer in Postmenopausal Women—Results from the MORE Trial. JAMA 1999; 281: 2189–2197
   PubMed Web of Science ®Google Scholar
• Gottardis M. M., Jordan V. C. The Antitumor Action of Keoxifene and Tamoxifen in the N-Nitrosomethylurea-Induced Rat Mammary Carcinoma Model. Cancer Res. 1987; 47: 4020–4024
   PubMed Web of Science ®Google Scholar
• Clemens J. A., Bennett D. R., Black L. J., et al. Effects of a New Antiestrogen, Keoxifene (LY156758), on Growth of Carcinogen-Induced Mammary Tumors and on LH and Prolactin Levels. Life Sci. 1983; 32: 2875
   Google Scholar
• Canavese G., Catturich A., Vecchio C., et al. Effects of Raloxifene on Serum Lipids and Coagulation Factors in Healthy Postmenopausal Women. JAMA 1998; 279: 1445–1451
   PubMed Web of Science ®Google Scholar
• Sato M., Turner C. H., Wang T., et al. LY353381.HCI: A Novel Raloxifene Analog with Improved SERM Potency and Efficacy In Vivo. J. Pharmacol. Exp. Ther. 1998; 287: 1–7
   PubMed Web of Science ®Google Scholar
• Tremblay A., Tremblay G. B., Labrie C., et al. EM-800, A Novel Antiestrogen, Acts as a Pure Antagonist of the Transcriptional Functions of Estrogen Receptors α and β. Endocrinology 1998; 139: 111–118
   PubMed Web of Science ®Google Scholar
• Luo S. Q., Labrie C., Belanger A., et al. Prevention of Development of Dimethylbenz(a)anthracene (DMBA)-Induced Mammary Tumors in the Rat by the New Nonsteroidal Antiestrogen EM-800 (SCH57050). Breast Cancer Res. Treat 1998; 49: 1–11
   PubMed Web of Science ®Google Scholar
• Rosati R. L., Jardine P. D., Cameron K. O., et al. Discovery and Preclinical Pharmacology of a Novel, Potent, Nonsteroidal Estrogen Receptor Agonist/Antagonist, CP-336156, a Diaryltetrahydronaphthalene. J. Med. Chem. 1998; 41: 2928–2931
   PubMed Web of Science ®Google Scholar
• Ke H. Z., Paralkar V. M., Grasser W. A., et al. Effects of CP-336,156, a New, Nonsteroidal Estrogen Agonist/ Antagonist, on Bone Serum Cholesterol, Uterus, and Body Composition in Rat Models. Endocrinology 1998; 139: 2068–2076
   PubMed Web of Science ®Google Scholar
• Gottardis M. M., Jiang S. Y., Jeng M. H., et al. Inhibition of Tamoxifen-Stimulated Growth of an MCF-7 Tumor Variant in Athymic Mice by Novel Steroidal Antiestrogens. Cancer Res. 1989; 49: 4090–4093
   PubMed Web of Science ®Google Scholar
• Osborne C. K., Coronado-Heinsohn E. B., Hilsenbeck S. G., et al. Comparison of the Effects of a Pure Steroidal Antiestrogen with Thoseof Tamoxifenin a Model ofHuman Breast Cancer. J. Natl. Cancer Inst. 1995; 87: 746–750
   PubMed Web of Science ®Google Scholar
• Tora L., White J., Brou C., et al. The Human Estrogen Receptor Has Two Independent Nonacidic Transcriptional Activation Functions. Cell 1989; 59: 477–487
   PubMed Web of Science ®Google Scholar
• Norris J. D., Fan D. J., Kerner S. A., et al. Identification of a Third Autonomous Activation Domain Within the Human Estrogen Receptor. Mol. Endocrinol. 1997; 11: 747–754
   PubMed Web of Science ®Google Scholar
• Berry M., Metzger D., Chambon P. Role of the Two Activating Domains of the Estrogen Receptor in the Cell-Type and Promoter-Context Dependent Agonist Activity of the Antiestrogen 4-Hydroxytamoxifen. EMBO J. 1990; 9: 2811–2818
   PubMed Web of Science ®Google Scholar
• Brzozowski A. M., Pike A. C.W., Dauter Z., et al. Molecular Basis of Agonism and Antagonism in the Oestrogen Receptor. Nature 1997; 389: 753–758
   PubMed Web of Science ®Google Scholar
• Grese T. A., Sluka J. P., Bryant H. U., et al. Molecular Determinants of Tissue Selectivity in Estrogen Receptor Modulators. Proc. Natl. Acad. Sci. U.S.A. 1997; 94: 14105–14110
   PubMed Web of Science ®Google Scholar
• Jackson T. A., Richer J. K., Bain D. L., et al. The Partial Agonist Activity of Antagonist-Occupied Steroid Receptors Is Controlled by a Novel Hinge Domain-Binding Coactivator L7/SPA and the Corepressors N-CoR or SMRT. Mol. Endocrinol. 1997; 11: 693–705
   PubMed Web of Science ®Google Scholar
• Smith C. L., Nawaz Z., O'Malley B. W., et al. Coactivator and Corepressor Regulation of the Agonist/Antagonist Activity of the Mixed Antiestrogen, 4-Hydroxytamoxifen. Mol. Endocrinol. 1997; 11: 657–666
   PubMed Web of Science ®Google Scholar
• Anzick S. L., Kononen J., Walker R. L., et al. AIB1, A Steroid Receptor Coactivator Amplified in Breast and Ovarian Cancer. Science 1997; 277: 965–968
   PubMed Web of Science ®Google Scholar
• Paech K., Webb P., Kuiper G. G.J.M., et al. Differential Activation of Estrogen Receptors ERα and ERβ at AP1 Sites. Science 1997; 277: 1508–1510
   PubMed Web of Science ®Google Scholar
• Hulley S., Grady D., Bush T., et al. Randomized Trial of Estrogen Plus Progestin for Secondary Prevention of Coronary Heart Disease in Postmenopausal Women. JAMA 1998; 280: 605–613
   PubMed Web of Science ®Google Scholar
• Dhingra K. Antiestrogens—Tamoxifen, SERMs and Beyond. Invest. New Drugs 1999; 17: 285–311
   PubMed Web of Science ®Google Scholar