The molecular, cellular and clinical consequences of targeting the estrogen receptor following estrogen deprivation therapy

Molecular and Cellular Endocrinology

Volumn 418, Issue , 2015, Pages 245-263

  Fan, Ping ^a   Maximov, Philipp Y ^a   Curpan, Ramona F ^b   Abderrahman, Balkees ^c   Jordan, V Craig ^a  

^a UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

^b ACADEMY OF ROMANIAN SCIENTISTS   (Romania)

^c UNIVERSITY OF JORDAN   (Jordan)

Author keywords

Antiestrogens; Breast cancer; Estrogen receptor; Estrogen induced apoptosis; Estrogens; Resistance

Indexed keywords

AFIMOXIFENE; BAZEDOXIFENE; CONJUGATED ESTROGEN; ENDOXIFEN; EPIDERMAL GROWTH FACTOR RECEPTOR 2; ESTROGEN RECEPTOR ALPHA; FULVESTRANT; GESTAGEN; LASOFOXIFENE; LETROZOLE; MEDROXYPROGESTERONE; OSPEMIFENE; PHYTOESTROGEN; PLACEBO; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; SOMATOMEDIN C RECEPTOR; TAMOXIFEN; ESTROGEN; ESTROGEN RECEPTOR; MEDROXYPROGESTERONE ACETATE; NANDROLONE;

APOPTOSIS; BREAST CANCER; CANCER INCIDENCE; CANCER PALLIATIVE THERAPY; CANCER PREVENTION; CANCER RESISTANCE; CANCER RISK; CLINICAL TRIAL (TOPIC); DRUG EFFECT; DRUG EFFICACY; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG TARGETING; DYSPAREUNIA; ESTROGEN RECEPTOR POSITIVE BREAST CANCER; ESTROGEN THERAPY; GENE MUTATION; HIGH RISK POPULATION; HORMONE SUBSTITUTION; HUMAN; LONG TERM CARE; MENOPAUSAL SYNDROME; META ANALYSIS (TOPIC); MOLECULAR MODEL; NONHUMAN; OSTEOPOROSIS; POSTMENOPAUSE; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN PROTEIN INTERACTION; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVIEW; RISK REDUCTION; SIGNAL TRANSDUCTION; BREAST NEOPLASMS; DRUG EFFECTS; DRUG RESISTANCE; FEMALE; GENETICS; METABOLISM; MUTATION;

APOPTOSIS; BREAST NEOPLASMS; DRUG RESISTANCE, NEOPLASM; ESTROGENS; FEMALE; HUMANS; MEDROXYPROGESTERONE ACETATE; MUTATION; NANDROLONE; RECEPTORS, ESTROGEN;

EID: 84949625158     PISSN: 03037207     EISSN: 18728057     Source Type: Journal    
DOI: 10.1016/j.mce.2015.06.004     Document Type: Review

References (225)

1. Allen E., Doisy E.A. An ovarian hormone. J. Am. Med. Assoc 1923, 81:819-821.
2. Anderson G.L., Limacher M., Assaf A.R., Bassford T., Beresford S.A., Black H., et al. Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women's Health Initiative randomized controlled trial. JAMA 2004, 291:1701-1712.
3. Anderson G.L., Chlebowski R.T., Aragaki A.K., Kuller L.H., Manson J.E., Gass M., et al. Conjugated equine oestrogen and breast cancer incidence and mortality in postmenopausal women with hysterectomy: extended follow-up of the Women's Health Initiative randomised placebo-controlled trial. Lancet Oncol 2012, 13:476-486.
4. Ariazi E.A., Cunliffe H.E., Lewis-Wambi J.S., Slifker M.J., Willis A.L., Ramos P., et al. Estrogen induces apoptosis in estrogen deprivation-resistant breast cancer through stress responses as identified by global gene expression across time. Proc. Natl. Acad. Sci. U.S.A. 2011, 108:18879-18886.
5. Balaburski G.M., Dardes R.C., Johnson M., Haddad B., Zhu F., Ross E.A., et al. Raloxifene-stimulated experimental breast cancer with the paradoxical actions of estrogen to promote or prevent tumor growth: a unifying concept in anti-hormone resistance. Int. J. Oncol 2010, 37:387-398.
6. Baum M. Use of aromatase inhibitors in the adjuvant treatment of breast cancer. Endocr. Relat. Cancer 1999, 6:231-234.
7. Baum M., Brinkley D.M., Dossett J.A., McPherson K., Patterson J.S., Rubens R.D., et al. Improved survival among patients treated with adjuvant tamoxifen after mastectomy for early breast cancer. Lancet 1983, 2:450.
8. Baum M., Budzar A.U., Cuzick J., Forbes J., Houghton J.H., Klijn J.G., et al. Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first results of the ATAC randomised trial. Lancet 2002, 359:2131-2139.
9. Beatson G.T. On the treatment of inoperable cases of carcinoma of the mamma: suggestions for a new method of treatment, with illustrative cases. Lancet 1896, 2:104-107.
10. Bentrem D., Fox J.E., Pearce S.T., Liu H., Pappas S., Kupfer D., et al. Distinct molecular conformations of the estrogen receptor alpha complex exploited by environmental estrogens. Cancer Res 2003, 63:7490-7496.
11. Beral V., Bull D., Reeves G. Endometrial cancer and hormone-replacement therapy in the Million Women Study. Lancet 2005, 365:1543-1551. Million Women Study Collaborators.
12. Beral V., Reeves G., Bull D., Green J. Breast cancer risk in relation to the interval between menopause and starting hormone therapy. J. Natl. Cancer Inst 2011, 103:296-305. Million Women Study Collaborators.
13. Berthois Y., Katzenellenbogen J.A., Katzenellenbogen B.S. Phenol red in tissue culture media is a weak estrogen: implications concerning the study of estrogen-responsive cells in culture. Proc. Natl. Acad. Sci. U.S.A. 1986, 83:2496-2500.
14. Boccardo F., Rubagotti A., Puntoni M., Guglielmini P., Amoroso D., Fini A., et al. Switching to anastrozole versus continued tamoxifen treatment of early breast cancer: preliminary results of the Italian Tamoxifen Anastrozole Trial. J. Clin. Oncol 2005, 23:5138-5147.
15. Boyd S. On oopherectomy in the cancer of the breast. Br. Med. J. 1900, ii:1161-1167.
16. Brzozowski A.M., Pike A.C., Dauter Z., Hubbard R.E., Bonn T., Engstrom O., et al. Molecular basis of agonism and antagonism in the oestrogen receptor. Nature 1997, 389:753-758.
17. Burstein H.J., Prestrud A.A., Seidenfeld J., Anderson H., Buchholz T.A., Davidson N.E., et al. American Society of Clinical Oncology clinical practice guideline: update on adjuvant endocrine therapy for women with hormone receptor-positive breast cancer. J. Clin. Oncol 2010, 28:3784-3796.
18. Burstein H.J., Temin S., Anderson H., Buchholz T.A., Davidson N.E., Gelmon K.E., et al. Adjuvant endocrine therapy for women with hormone receptor-positive breast cancer: American Society of Clinical Oncology clinical practice guideline focused update. J. Clin. Oncol 2014, 32:2255-2269.
19. Catherino W.H., Jeng M.H., Jordan V.C. Norgestrel and gestodene stimulate breast cancer cell growth through an oestrogen receptor mediated mechanism. Br. J. Cancer 1993, 67:945-952.
20. Catherino W.H., Wolf D.M., Jordan V.C. A naturally occurring estrogen receptor mutation results in increased estrogenicity of a tamoxifen analog. Mol. Endocrinol 1995, 9:1053-1063.
21. Cauley J.A., Norton L., Lippman M.E., Eckert S., Krueger K.A., Purdie D.W., et al. Continued breast cancer risk reduction in postmenopausal women treated with raloxifene: 4-year results from the MORE trial. Multiple outcomes of raloxifene evaluation. Breast Cancer Res. Treat 2001, 65:125-134.
22. Chang C.Y., Norris J.D., Gron H., Paige L.A., Hamilton P.T., Kenan D.J., et al. Dissection of the LXXLL nuclear receptor-coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta. Mol. Cell. Biol 1999, 19:8226-8239.
23. Chen M., Rao Y., Zheng Y., Wei S., Li Y., Guo T., et al. Association between soy isoflavone intake and breast cancer risk for pre- and post-menopausal women: a meta-analysis of epidemiological studies. PLoS ONE 2014, 9:e89288.
24. Chlebowski R.T., Rohan T.E., Manson J.E., Aragaki A.K., Kaunitz A., Stefanick M.L., et al. Breast cancer after use of estrogen plus progestin and estrogen alone: analyses of data from 2 women's health initiative randomized clinical trials. JAMA Oncol 2015, 10.1001/jamaoncol.2015.0494.
25. Chobert M.N., Barouki R., Finidori J., Aggerbeck M., Hanoune J., Philibert D., et al. Antiglucocorticoid properties of RU 38486 in a differentiated hepatoma cell line. Biochem. Pharmacol 1983, 32:3481-3483.
26. Coates A.S., Keshaviah A., Thurlimann B., Mouridsen H., Mauriac L., Forbes J.F., et al. Five years of letrozole compared with tamoxifen as initial adjuvant therapy for postmenopausal women with endocrine-responsive early breast cancer: update of study BIG 1-98. J. Clin. Oncol 2007, 25:486-492.
27. Coombes R.C., Goss P., Dowsett M., Gazet J.C., Brodie A. 4-Hydroxyandrostenedione in treatment of postmenopausal patients with advanced breast cancer. Lancet 1984, 2:1237-1239.
28. Coombes R.C., Hall E., Gibson L.J., Paridaens R., Jassem J., Delozier T., et al. A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer. N. Engl. J. Med 2004, 350:1081-1092.
29. Cummings F.J., Gray R., Davis T.E., Tormey D.C., Harris J.E., Falkson G., et al. Adjuvant tamoxifen treatment of elderly women with stage II breast cancer. A double-blind comparison with placebo. Ann. Intern. Med 1985, 103:324-329.
30. Cummings S.R., Eckert S., Krueger K.A., Grady D., Powles T.J., Cauley J.A., et al. The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. JAMA 1999, 281:2189-2197.
31. Cuzick J., Baum M. Tamoxifen and contralateral breast cancer. Lancet 1985, 2:282.
32. Cuzick J., Forbes J.F., Sestak I., Cawthorn S., Hamed H., Holli K., et al. Long-term results of tamoxifen prophylaxis for breast cancer-96-month follow-up of the randomized IBIS-I trial. J. Natl. Cancer Inst 2007, 99:272-282.
33. Cuzick J., Sestak I., Baum M., Buzdar A., Howell A., Dowsett M., et al. Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 10-year analysis of the ATAC trial. Lancet Oncol 2010, 11:1135-1141.
34. Davies C., Pan H., Godwin J., Gray R., Arriagada R., Raina V., et al. Long-term effects of continuing adjuvant tamoxifen to 10 years versus stopping at 5 years after diagnosis of oestrogen receptor-positive breast cancer: ATLAS, a randomised trial. Lancet 2013, 381:805-816.
35. Delozier T., Julien J.P., Juret P., Veyret C., Couette J.E., Graic Y., et al. Adjuvant tamoxifen in postmenopausal breast cancer: preliminary results of a randomized trial. Breast Cancer Res. Treat 1986, 7:105-109.
36. Di Leo A., Jerusalem G., Petruzelka L., Torres R., Bondarenko I.N., Khasanov R., et al. Final overall survival: fulvestrant 500 mg vs 250 mg in the randomized CONFIRM trial. J. Natl. Cancer Inst 2014, 106:djt337.
37. Dowsett M., Cuzick J., Ingle J., Coates A., Forbes J., Bliss J., et al. Meta-analysis of breast cancer outcomes in adjuvant trials of aromatase inhibitors versus tamoxifen. J. Clin. Oncol 2010, 28:509-518.
38. DuSell C.D., Umetani M., Shaul P.W., Mangelsdorf D.J., McDonnell D.P. 27-Hydroxycholesterol is an endogenous selective estrogen receptor modulator. Mol. Endocrinol 2008, 22:65-77.
39. DuSell C.D., Nelson E.R., Wang X., Abdo J., Modder U.I., Umetani M., et al. The endogenous selective estrogen receptor modulator 27-hydroxycholesterol is a negative regulator of bone homeostasis. Endocrinology 2010, 151:3675-3685.
40. EBCTCG Tamoxifen for early breast cancer: an overview of the randomised trials. Lancet 1998, 351:1451-1467.
41. EBCTCG Effects of chemotherapy and hormonal therapy for early breast cancer on recurrence and 15-year survival: an overview of the randomised trials. Lancet 2005, 365:1687-1717.
42. EBCTCG Relevance of breast cancer hormone receptors and other factors to the efficacy of adjuvant tamoxifen: patient-level meta-analysis of randomised trials. Lancet 2011, 378:771-784.
43. Ellis M.J., Gao F., Dehdashti F., Jeffe D.B., Marcom P.K., Carey L.A., et al. Lower-dose vs high-dose oral estradiol therapy of hormone receptor-positive, aromatase inhibitor-resistant advanced breast cancer: a phase 2 randomized study. JAMA 2009, 302:774-780.
44. Fagan D.H., Uselman R.R., Sachdev D., Yee D. Acquired resistance to tamoxifen is associated with loss of the type I insulin-like growth factor receptor: implications for breast cancer treatment. Cancer Res 2012, 72:3372-3380.
45. Falkson H.C., Gray R., Wolberg W.H., Gillchrist K.W., Harris J.E., Tormey D.C., et al. Adjuvant trial of 12 cycles of CMFPT followed by observation or continuous tamoxifen versus four cycles of CMFPT in postmenopausal women with breast cancer: an Eastern Cooperative Oncology Group phase III study. J. Clin. Oncol 1990, 8:599-607.
46. Fan P., Wang J., Santen R.J., Yue W. Long-term treatment with tamoxifen facilitates translocation of estrogen receptor alpha out of the nucleus and enhances its interaction with EGFR in MCF-7 breast cancer cells. Cancer Res 2007, 67:1352-1360.
47. Fan P., McDaniel R.E., Kim H.R., Clagett D., Haddad B., Jordan V.C. Modulating therapeutic effects of the c-Src inhibitor via oestrogen receptor and human epidermal growth factor receptor 2 in breast cancer cell lines. Eur. J. Cancer 2012, 48:3488-3498.
48. Fan P., Griffith O.L., Agboke F.A., Anur P., Zou X., McDaniel R.E., et al. c-Src modulates estrogen-induced stress and apoptosis in estrogen-deprived breast cancer cells. Cancer Res 2013, 73:4510-4520.
49. Fan P., Cunliffe H.E., Griffith O.L., Agboke F.A., Ramos P., Gray J.W., et al. Identification of gene regulation patterns underlying both oestrogen- and tamoxifen-stimulated cell growth through global gene expression profiling in breast cancer cells. Eur. J. Cancer 2014, 50:2877-2886.
50. Fan P., Agboke F.A., Cunliffe H.E., Ramos P., Jordan V.C. A molecular model for the mechanism of acquired tamoxifen resistance in breast cancer. Eur. J. Cancer 2014, 50:2866-2876.
51. Fan P., Agboke F.A., McDaniel R.E., Sweeney E.E., Zou X., Creswell K., et al. Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur. J. Cancer 2014, 50:457-468.
52. Feng W., Webb P., Nguyen P., Liu X., Li J., Karin M., et al. Potentiation of estrogen receptor activation function 1 (AF-1) by Src/JNK through a serine 118-independent pathway. Mol. Endocrinol 2001, 15:32-45.
53. Ferlay J., Soerjomataram I., Ervik M., Dikshit R., Eser S., Mathers C., et al. GLOBOCAN 2012 v1.0, Cancer Incidence and Mortality Worldwide: IARC CancerBase No. 11. 2013, International Agency for Research on Cancer, Lyon, France, Available from. http://globocan.iarc.fr.
54. Fisher B., Redmond C., Brown A., Fisher E.R., Wolmark N., Bowman D., et al. Adjuvant chemotherapy with and without tamoxifen in the treatment of primary breast cancer: 5-year results from the National Surgical Adjuvant Breast and Bowel Project Trial. J. Clin. Oncol 1986, 4:459-471.
55. Fisher B., Brown A., Wolmark N., Redmond C., Wickerham D.L., Wittliff J., et al. Prolonging tamoxifen therapy for primary breast cancer. Findings from the National Surgical Adjuvant Breast and Bowel Project clinical trial. Ann. Intern. Med 1987, 106:649-654.
56. Fisher B., Dignam J., Bryant J., DeCillis A., Wickerham D.L., Wolmark N., 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.
57. Fisher B., Costantino J.P., Wickerham D.L., Redmond C.K., Kavanah M., Cronin W.M., 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.
58. Fisher B., Costantino J.P., Wickerham D.L., Cecchini R.S., Cronin W.M., Robidoux A., et al. Tamoxifen for the prevention of breast cancer: current status of the National Surgical Adjuvant Breast and Bowel Project P-1 study. J. Natl. Cancer Inst 2005, 97:1652-1662.
59. Folca P.J., Glascock R.F., Irvine W.T. Studies with tritium-labelled hexoestrol in advanced breast cancer. Comparison of tissue accumulation of hexoestrol with response to bilateral adrenalectomy and oophorectomy. Lancet 1961, 2:796-798.
60. Forbes J.F., Cuzick J., Buzdar A., Howell A., Tobias J.S., Baum M. Effect of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer: 100-month analysis of the ATAC trial. Lancet Oncol 2008, 9:45-53.
61. Fornander T., Rutqvist L.E., Cedermark B., Glas U., Mattsson A., Silfversward C., et al. Adjuvant tamoxifen in early breast cancer: occurrence of new primary cancers. Lancet 1989, 1:117-120.
62. Glascock R.F., Hoekstra W.G. Selective accumulation of tritium-labelled hexoestrol by the reproductive organs of immature female goats and sheep. Biochem. J. 1959, 72:673-682.
63. Goss P.E., Ingle J.N., Martino S., Robert N.J., Muss H.B., Piccart M.J., et al. A randomized trial of letrozole in postmenopausal women after five years of tamoxifen therapy for early-stage breast cancer. N. Engl. J. Med 2003, 349:1793-1802.
64. Goss P.E., Ingle J.N., Martino S., Robert N.J., Muss H.B., Piccart M.J., et al. Randomized trial of letrozole following tamoxifen as extended adjuvant therapy in receptor-positive breast cancer: updated findings from NCIC CTG MA.17. J. Natl. Cancer Inst 2005, 97:1262-1271.
65. 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.
66. Gottardis M.M., Robinson S.P., Satyaswaroop P.G., Jordan V.C. Contrasting actions of tamoxifen on endometrial and breast tumor growth in the athymic mouse. Cancer Res 1988, 48:812-815.
67. Gottardis M.M., Wagner R.J., Borden E.C., Jordan V.C. Differential ability of antiestrogens to stimulate breast cancer cell (MCF-7) growth in vivo and in vitro. Cancer Res 1989, 49:4765-4769.
68. Gottardis M.M., Jiang S.Y., Jeng M.H., Jordan V.C. Inhibition of tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic mice by novel steroidal antiestrogens. Cancer Res 1989, 49:4090-4093.
69. Gradishar W.J., Jordan V.C. Clinical potential of new antiestrogens. J. Clin. Oncol 1997, 15:840-852.
70. Greene G.L., Gilna P., Waterfield M., Baker A., Hort Y., Shine J. Sequence and expression of human estrogen receptor complementary DNA. Science 1986, 231:1150-1154.
71. Haddow A. David A. Karnofsky memorial lecture. Thoughts on chemical therapy. Cancer 1970, 26:737-754.
72. Haddow A., Watkinson J.M., Paterson E. Influence of synthetic oestrogens upon advanced malignant disease. Br. Med. J. 1944, 2:393-398.
73. Haldosen L.A., Zhao C., Dahlman-Wright K. Estrogen receptor beta in breast cancer. Mol. Cell. Endocrinol 2014, 382:665-672.
74. Hardell L. Tamoxifen as risk factor for carcinoma of corpus uteri. Lancet 1988, 2:563.
75. Harper M.J., Walpole A.L. A new derivative of triphenylethylene: effect on implantation and mode of action in rats. J. Reprod. Fertil 1967, 13:101-119.
76. Howell A., Dodwell D.J., Anderson H., Redford J. Response after withdrawal of tamoxifen and progestogens in advanced breast cancer. Ann. Oncol 1992, 3:611-617.
77. Howell A., Robertson J.F., Quaresma Albano J., Aschermannova A., Mauriac L., Kleeberg U.R., et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. J. Clin. Oncol 2002, 20:3396-3403.
78. Howell A., Cuzick J., Baum M., Buzdar A., Dowsett M., Forbes J.F., et al. Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial after completion of 5 years' adjuvant treatment for breast cancer. Lancet 2005, 365:60-62.
79. Huang H.J., Norris J.D., McDonnell D.P. Identification of a negative regulatory surface within estrogen receptor alpha provides evidence in support of a role for corepressors in regulating cellular responses to agonists and antagonists. Mol. Endocrinol 2002, 16:1778-1792.
80. Hutcheson I.R., Knowlden J.M., Madden T.A., Barrow D., Gee J.M., Wakeling A.E., et al. Oestrogen receptor-mediated modulation of the EGFR/MAPK pathway in tamoxifen-resistant MCF-7 cells. Breast Cancer Res. Treat 2003, 81:81-93.
81. Jeng M.H., Parker C.J., Jordan V.C. Estrogenic potential of progestins in oral contraceptives to stimulate human breast cancer cell proliferation. Cancer Res 1992, 52:6539-6546.
82. Jeng M.H., Jiang S.Y., Jordan V.C. Paradoxical regulation of estrogen-dependent growth factor gene expression in estrogen receptor (ER)-negative human breast cancer cells stably expressing ER. Cancer Lett 1994, 82:123-128.
83. Jensen E.V., Jacobson H.I. Basic guides to the mechanism of estrogen action. Recent Prog. Horm. Res 1962, 18:387-414.
84. Jensen E.V., Jordan V.C. The estrogen receptor: a model for molecular medicine. Clin. Cancer Res 2003, 9:1980-1989.
85. Jensen E.V., Block G.E., Smith S., Kyser K., DeSombre E.R. Estrogen receptors and breast cancer response to adrenalectomy. Natl. Cancer Inst. Monogr 1971, 34:55-70.
86. Jeselsohn R., Yelensky R., Buchwalter G., Frampton G., Meric-Bernstam F., Gonzalez-Angulo A.M., et al. Emergence of constitutively active estrogen receptor-alpha mutations in pretreated advanced estrogen receptor-positive breast cancer. Clin. Cancer Res 2014, 20:1757-1767.
87. Jiang S.Y., Jordan V.C. Growth regulation of estrogen receptor-negative breast cancer cells transfected with complementary DNAs for estrogen receptor. J. Natl. Cancer Inst 1992, 84:580-591.
88. Jordan V.C. Use of DMBA-induced rat mammary carcinoma system for the evaluation of tamoxifen as a potential adjuvant therapy. Rev. Endocr. Relat. Cancer 1978, (October Suppl.):49-55.
89. Jordan V.C. Laboratory studies to develop general principles for the adjuvant treatment of breast cancer with antiestrogens: problems and potential for future clinical applications. Breast Cancer Res. Treat 1983, 3(Suppl.):S73-S86.
90. Jordan V.C. Biochemical pharmacology of antiestrogen action. Pharmacol. Rev 1984, 36:245-276.
91. Jordan V.C. Laboratory models of breast cancer to aid the elucidation of antiestrogen action. J. Lab. Clin. Med 1987, 109:267-277.
92. Jordan V.C. Chemosuppression of breast cancer with tamoxifen: laboratory evidence and future clinical investigations. Cancer Invest 1988, 6:589-595.
93. Jordan V.C. Tamoxifen and endometrial cancer. Lancet 1988, 2:1019.
94. Jordan V.C. Antiestrogenic action of raloxifene and tamoxifen: today and tomorrow. J. Natl. Cancer Inst 1998, 90:967-971.
95. Jordan V.C. Selective estrogen receptor modulation: a personal perspective. Cancer Res 2001, 61:5683-5687.
96. Jordan V.C. Tamoxifen: a most unlikely pioneering medicine. Nat. Rev. Drug Discov 2003, 2:205-213.
97. Jordan V.C. Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions. J. Med. Chem 2003, 46:883-908.
98. Jordan V.C. Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents. J. Med. Chem 2003, 46:1081-1111.
99. Jordan V.C. Selective estrogen receptor modulation: concept and consequences in cancer. Cancer Cell 2004, 5:207-213.
100. Jordan V.C. Tamoxifen (ICI46,474) as a targeted therapy to treat and prevent breast cancer. Br. J. Pharmacol 2006, 147(Suppl. 1):S269-S376.
101. Jordan V.C. Chemoprevention of breast cancer with selective oestrogen-receptor modulators. Nat. Rev. Cancer 2007, 7:46-53.
102. Jordan V.C. Tamoxifen: catalyst for the change to targeted therapy. Eur. J. Cancer 2008, 44:30-38.
103. Jordan V.C. The 38th David A. Karnofsky lecture: the paradoxical actions of estrogen in breast cancer-survival or death?. J. Clin. Oncol 2008, 26:3073-3082.
104. Jordan V.C. Tamoxifen as the first targeted long-term adjuvant therapy for breast cancer. Endocr. Relat. Cancer 2014, 21:R235-R246.
105. Jordan V.C. Linking estrogen-induced apoptosis with decreases in mortality following long-term adjuvant tamoxifen therapy. J. Natl. Cancer Inst 2014, 106. 10.1093/jnci/dju296.
106. Jordan V.C. Avoiding the bad and enhancing the good of soy supplements in breast cancer. J. Natl. Cancer Inst 2014, 106. 10.1093/jnci/dju233.
107. Jordan V.C. Proven value of translational research with appropriate animal models to advance breast cancer treatment and save lives: the tamoxifen tale. Br. J. Clin. Pharmacol 2015, 79:254-267.
108. Jordan V.C. The new biology of estrogen-induced apoptosis applied to treat and prevent breast cancer. Endocr. Relat. Cancer 2015, 22:R1-R31.
109. Jordan V.C., Allen K.E. Evaluation of the antitumour activity of the non-steroidal antioestrogen monohydroxytamoxifen in the DMBA-induced rat mammary carcinoma model. Eur. J. Cancer 1980, 16:239-251.
110. Jordan V.C., Brodie A.M. Development and evolution of therapies targeted to the estrogen receptor for the treatment and prevention of breast cancer. Steroids 2007, 72:7-25.
111. Jordan V.C., Ford L.G. Paradoxical clinical effect of estrogen on breast cancer risk: a "new" biology of estrogen-induced apoptosis. Cancer Prev. Res. (Phila.) 2011, 4:633-637.
112. Jordan V.C., Koch R. Regulation of prolactin synthesis in vitro by estrogenic and antiestrogenic derivatives of estradiol and estrone. Endocrinology 1989, 124:1717-1726.
113. Jordan V.C., O'Malley B.W. Selective estrogen-receptor modulators and antihormonal resistance in breast cancer. J. Clin. Oncol 2007, 25:5815-5824.
114. Jordan V.C., Dix C.J., Allen K.E. The effectiveness of long term tamoxifen treatment in a laboratory model for adjuvant hormone therapy of breast cancer. Adjuvant Therapy of Cancer II 1979, 19-26. Grune & Stratton Inc., New York. S.E. Salmon, S.E. Jones (Eds.).
115. Jordan V.C., Lieberman M.E., Cormier E., Koch R., Bagley J.R., Ruenitz P.C. Structural requirements for the pharmacological activity of nonsteroidal antiestrogens in vitro. Mol. Pharmacol 1984, 26:272-278.
116. Jordan V.C., Koch R., Mittal S., Schneider M.R. Oestrogenic and antioestrogenic actions in a series of triphenylbut-1-enes: modulation of prolactin synthesis in vitro. Br. J. Pharmacol 1986, 87:217-223.
117. Jordan V.C., Phelps E., Lindgren J.U. Effects of anti-estrogens on bone in castrated and intact female rats. Breast Cancer Res. Treat 1987, 10:31-35.
118. Jordan V.C., Wolf M.F., Mirecki D.M., Whitford D.A., Welshons W.V. Hormone receptor assays: clinical usefulness in the management of carcinoma of the breast. Crit. Rev. Clin. Lab. Sci 1988, 26:97-152.
119. Jordan V.C., Schafer J.M., Levenson A.S., Liu H., Pease K.M., Simons L.A., et al. Molecular classification of estrogens. Cancer Res 2001, 61:6619-6623.
120. Jordan V.C., Curpan R.F., Maximov P.Y. Estrogen receptor (ER) mutations found in breast cancer metastases integrated with the molecular pharmacology of selective ER modulators (SERMs). J. Natl. Cancer Inst 2015, 107(6). 10.1093/jnci/djv075.
121. Kalaitzidis D., Gilmore T.D. Transcription factor cross-talk: the estrogen receptor and NF-kappaB. Trends Endocrinol. Metab 2005, 16:46-52.
122. Kennedy B.J., Nathanson I.T. Effects of intensive sex steroid hormone therapy in advanced breast cancer. J. Am. Med. Assoc 1953, 152:1135-1141.
123. Klinge C.M. Estrogen receptor interaction with estrogen response elements. Nucleic Acids Res 2001, 29:2905-2919.
124. Knowlden J.M., Hutcheson I.R., Barrow D., Gee J.M., Nicholson R.I. Insulin-like growth factor-I receptor signaling in tamoxifen-resistant breast cancer: a supporting role to the epidermal growth factor receptor. Endocrinology 2005, 146:4609-4618.
125. Koide A., Zhao C., Naganuma M., Abrams J., Deighton-Collins S., Skafar D.F., et al. Identification of regions within the F domain of the human estrogen receptor alpha that are important for modulating transactivation and protein-protein interactions. Mol. Endocrinol 2007, 21:829-842.
126. Koubovec D., Ronacher K., Stubsrud E., Louw A., Hapgood J.P. Synthetic progestins used in HRT have different glucocorticoid agonist properties. Mol. Cell. Endocrinol 2005, 242:23-32.
127. Kuiper G.G., Enmark E., Pelto-Huikko M., Nilsson S., Gustafsson J.A. Cloning of a novel receptor expressed in rat prostate and ovary. Proc. Natl. Acad. Sci. U.S.A. 1996, 93:5925-5930.
128. Kumar V., Green S., Stack G., Berry M., Jin J.R., Chambon P. Functional domains of the human estrogen receptor. Cell 1987, 51:941-951.
129. Lacassagne A. A comparative study of the carcinogenic action of certain oestrogenic hormones. Am. J. Cancer 1936, 28:735-740.
130. Lacassagne A. Hormonal pathogenesis of adenocarcinoma of the breast. Am. J. Cancer 1936, 27:217-228.
131. Lannigan D.A. Estrogen receptor phosphorylation. Steroids 2003, 68:1-9.
132. Lathrop A.E., Loeb L. Further investigations on the origin of tumors in mice. III. On the part played by internal secretion in the spontaneous development of tumors. J. Cancer Res 1916, 1:1-19.
133. Lee E.S., Schafer J.M., Yao K., England G., O'Regan R.M., De Los Reyes A., et al. Cross-resistance of triphenylethylene-type antiestrogens but not ICI 182,780 in tamoxifen-stimulated breast tumors grown in athymic mice. Clin. Cancer Res 2000, 6:4893-4899.
134. Lerner L.J., Jordan V.C. Development of antiestrogens and their use in breast cancer: eighth Cain memorial award lecture. Cancer Res 1990, 50:4177-4189.
135. Levenson A.S., Jordan V.C. The key to the antiestrogenic mechanism of raloxifene is amino acid 351 (aspartate) in the estrogen receptor. Cancer Res 1998, 58:1872-1875.
136. Levenson A.S., Catherino W.H., Jordan V.C. Estrogenic activity is increased for an antiestrogen by a natural mutation of the estrogen receptor. J. Steroid Biochem. Mol. Biol 1997, 60:261-268.
137. Levenson A.S., Tonetti D.A., Jordan V.C. The oestrogen-like effect of 4-hydroxytamoxifen on induction of transforming growth factor alpha mRNA in MDA-MB-231 breast cancer cells stably expressing the oestrogen receptor. Br. J. Cancer 1998, 77:1812-1819.
138. Levenson A.S., MacGregor Schafer J.I., Bentrem D.J., Pease K.M., Jordan V.C. Control of the estrogen-like actions of the tamoxifen-estrogen receptor complex by the surface amino acid at position 351. J. Steroid Biochem. Mol. Biol 2001, 76:61-70.
139. Lewis J.S., Osipo C., Meeke K., Jordan V.C. Estrogen-induced apoptosis in a breast cancer model resistant to long-term estrogen withdrawal. J. Steroid Biochem. Mol. Biol 2005, 94:131-141.
140. Lewis J.S., Meeke K., Osipo C., Ross E.A., Kidawi N., Li T., et al. Intrinsic mechanism of estradiol-induced apoptosis in breast cancer cells resistant to estrogen deprivation. J. Natl. Cancer Inst 2005, 97:1746-1759.
141. Li S., Shen D., Shao J., Crowder R., Liu W., Prat A., et al. Endocrine-therapy-resistant ESR1 variants revealed by genomic characterization of breast-cancer-derived xenografts. Cell Rep 2013, 4:1116-1130.
142. Lieberman M.E., Jordan V.C., Fritsch M., Santos M.A., Gorski J. Direct and reversible inhibition of estradiol-stimulated prolactin synthesis by antiestrogens in vitro. J. Biol. Chem 1983, 258:4734-4740.
143. Lieberman M.E., Gorski J., Jordan V.C. An estrogen receptor model to describe the regulation of prolactin synthesis by antiestrogens in vitro. J. Biol. Chem 1983, 258:4741-4745.
144. Liu H., Lee E.S., Deb Los Reyes A., Zapf J.W., Jordan V.C. Silencing and reactivation of the selective estrogen receptor modulator-estrogen receptor alpha complex. Cancer Res 2001, 61:3632-3639.
145. Liu H., Park W.C., Bentrem D.J., McKian K.P., Reyes Ade L., Loweth J.A., et al. Structure-function relationships of the raloxifene-estrogen receptor-alpha complex for regulating transforming growth factor-alpha expression in breast cancer cells. J. Biol. Chem 2002, 277:9189-9198.
146. Liu H., Lee E.S., Gajdos C., Pearce S.T., Chen B., Osipo C., et al. Apoptotic action of 17beta-estradiol in raloxifene-resistant MCF-7 cells in vitro and in vivo. J. Natl. Cancer Inst 2003, 95:1586-1597.
147. Lonard D.M., Tsai S.Y., O'Malley B.W. Selective estrogen receptor modulators 4-hydroxytamoxifen and raloxifene impact the stability and function of SRC-1 and SRC-3 coactivator proteins. Mol. Cell. Biol 2004, 24:14-24.
148. Lonning P.E. Additive endocrine therapy for advanced breast cancer - back to the future. Acta Oncol 2009, 48:1092-1101.
149. Lonning P.E., Taylor P.D., Anker G., Iddon J., Wie L., Jorgensen L.M., et al. High-dose estrogen treatment in postmenopausal breast cancer patients heavily exposed to endocrine therapy. Breast Cancer Res. Treat 2001, 67:111-116.
150. Love R.R., Newcomb P.A., Wiebe D.A., Surawicz T.S., Jordan V.C., Carbone P.P., et al. Effects of tamoxifen therapy on lipid and lipoprotein levels in postmenopausal patients with node-negative breast cancer. J. Natl. Cancer Inst 1990, 82:1327-1332.
151. Love R.R., Wiebe D.A., Newcomb P.A., Cameron L., Leventhal H., Jordan V.C., et al. Effects of tamoxifen on cardiovascular risk factors in postmenopausal women. Ann. Intern. Med 1991, 115:860-864.
152. Love R.R., Mazess R.B., Barden H.S., Epstein S., Newcomb P.A., Jordan V.C., et al. Effects of tamoxifen on bone mineral density in postmenopausal women with breast cancer. N. Engl. J. Med 1992, 326:852-856.
153. MacGregor Schafer J., Liu H., Bentrem D.J., Zapf J.W., Jordan V.C. Allosteric silencing of activating function 1 in the 4-hydroxytamoxifen estrogen receptor complex is induced by substituting glycine for aspartate at amino acid 351. Cancer Res 2000, 60:5097-5105.
154. MacGregor Schafer J., Liu H., Levenson A.S., Horiguchi J., Chen Z., Jordan V.C. Estrogen receptor alpha mediated induction of the transforming growth factor alpha gene by estradiol and 4-hydroxytamoxifen in MDA-MB-231 breast cancer cells. J. Steroid Biochem. Mol. Biol 2001, 78:41-50.
155. Martino S., Cauley J.A., Barrett-Connor E., Powles T.J., Mershon J., Disch D., et al. Continuing outcomes relevant to Evista: breast cancer incidence in postmenopausal osteoporotic women in a randomized trial of raloxifene. J. Natl. Cancer Inst 2004, 96:1751-1761.
156. Massarweh S., Osborne C.K., Creighton C.J., Qin L., Tsimelzon A., Huang S., et al. Tamoxifen resistance in breast tumors is driven by growth factor receptor signaling with repression of classic estrogen receptor genomic function. Cancer Res 2008, 68:826-833.
157. Maximov P.Y., Myers C.B., Curpan R.F., Lewis-Wambi J.S., Jordan V.C. Structure-function relationships of estrogenic triphenylethylenes related to endoxifen and 4-hydroxytamoxifen. J. Med. Chem 2010, 53:3273-3283.
158. Maximov P.Y., Sengupta S., Lewis-Wambi J.S., Kim H.R., Curpan R.F., Jordan V.C. The conformation of the estrogen receptor directs estrogen-induced apoptosis in breast cancer: a hypothesis. Horm. Mol. Biol. Clin. Investig 2011, 5:27-34.
159. Maximov P.Y., McDaniel R.E., Jordan V.C. Tamoxifen: Pioneering Medicine in Breast Cancer 2013, Springer, Basel.
160. Maximov P.Y., Lee T.M., Jordan V.C. The discovery and development of selective estrogen receptor modulators (SERMs) for clinical practice. Curr. Clin. Pharmacol 2013, 8:135-155.
161. Maximov P.Y., Fernandes D.J., McDaniel R.E., Myers C.B., Curpan R.F., Jordan V.C. Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells. J. Med. Chem 2014, 57:4569-4583.
162. McDaniel R.E., Maximov P.Y., Jordan V.C. Estrogen-mediated mechanisms to control the growth and apoptosis of breast cancer cells: a translational research success story. Vitam. Horm 2013, 93:1-49.
163. McGuire W.L., Carbone P.P., Vollmer E.P. Estrogen Receptors in Human Breast Cancer 1975, Raven Press, New York.
164. McKenna N.J., O'Malley B.W. Minireview: nuclear receptor coactivators-an update. Endocrinology 2002, 143:2461-2465.
165. Merenbakh-Lamin K., Ben-Baruch N., Yeheskel A., Dvir A., Soussan-Gutman L., Jeselsohn R., et al. D538G mutation in estrogen receptor-alpha: a novel mechanism for acquired endocrine resistance in breast cancer. Cancer Res 2013, 73:6856-6864.
166. Montano M.M., Muller V., Trobaugh A., Katzenellenbogen B.S. The carboxy-terminal F domain of the human estrogen receptor: role in the transcriptional activity of the receptor and the effectiveness of antiestrogens as estrogen antagonists. Mol. Endocrinol 1995, 9:814-825.
167. Murphy C.S., Langan-Fahey S.M., McCague R., Jordan V.C. Structure-function relationships of hydroxylated metabolites of tamoxifen that control the proliferation of estrogen-responsive T47D breast cancer cells in vitro. Mol. Pharmacol 1990, 38:737-743.
168. Murphy C.S., Parker C.J., McCague R., Jordan V.C. Structure-activity relationships of nonisomerizable derivatives of tamoxifen: importance of hydroxyl group and side chain positioning for biological activity. Mol. Pharmacol 1991, 39:421-428.
169. Nagata C., Mizoue T., Tanaka K., Tsuji I., Tamakoshi A., Matsuo K., et al. Soy intake and breast cancer risk: an evaluation based on a systematic review of epidemiologic evidence among the Japanese population. Jpn. J. Clin. Oncol 2014, 44:282-295.
170. NATO Controlled trial of tamoxifen as adjuvant agent in management of early breast cancer. Interim analysis at four years by Nolvadex Adjuvant Trial Organisation. Lancet 1983, 1:257-261.
171. NATO Controlled trial of tamoxifen as single adjuvant agent in management of early breast cancer. Analysis at six years by Nolvadex Adjuvant Trial Organisation. Lancet 1985, 1:836-840.
172. Nelson E.R., Wardell S.E., Jasper J.S., Park S., Suchindran S., Howe M.K., et al. 27-Hydroxycholesterol links hypercholesterolemia and breast cancer pathophysiology. Science 2013, 342:1094-1098.
173. Norris J.D., Paige L.A., Christensen D.J., Chang C.Y., Huacani M.R., Fan D., et al. Peptide antagonists of the human estrogen receptor. Science 1999, 285:744-746.
174. Obiorah I., Jordan V.C. Scientific rationale for postmenopause delay in the use of conjugated equine estrogens among postmenopausal women that causes reduction in breast cancer incidence and mortality. Menopause 2013, 20:372-382.
175. Obiorah I., Sengupta S., Curpan R., Jordan V.C. Defining the conformation of the estrogen receptor complex that controls estrogen-induced apoptosis in breast cancer. Mol. Pharmacol 2014, 85:789-799.
176. Obiorah I., Sengupta S., Fan P., Jordan V.C. Delayed triggering of oestrogen induced apoptosis that contrasts with rapid paclitaxel-induced breast cancer cell death. Br. J. Cancer 2014, 110:1488-1496.
177. Obiorah I.E., Jordan V.C. Differences in the rate of oestrogen-induced apoptosis in breast cancer by oestradiol and the triphenylethylene bisphenol. Br. J. Pharmacol 2014, 171:4062-4072.
178. Obiorah I.E., Fan P., Jordan V.C. Breast cancer cell apoptosis with phytoestrogens is dependent on an estrogen-deprived state. Cancer Prev. Res. (Phila.) 2014, 7:939-949.
179. Onate S.A., Tsai S.Y., Tsai M.J., O'Malley B.W. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily. Science 1995, 270:1354-1357.
180. Osborne C.K., Pippen J., Jones S.E., Parker L.M., Ellis M., Come S., et al. Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial. J. Clin. Oncol 2002, 20:3386-3395.
181. Osipo C., Gajdos C., Liu H., Chen B., Jordan V.C. Paradoxical action of fulvestrant in estradiol-induced regression of tamoxifen-stimulated breast cancer. J. Natl. Cancer Inst 2003, 95:1597-1608.
182. Osipo C., Meeke K., Cheng D., Weichel A., Bertucci A., Liu H., et al. Role for HER2/neu and HER3 in fulvestrant-resistant breast cancer. Int. J. Oncol 2007, 30:509-520.
183. Powles T.J., Ashley S., Tidy A., Smith I.E., Dowsett M. Twenty-year follow-up of the Royal Marsden randomized, double-blinded tamoxifen breast cancer prevention trial. J. Natl. Cancer Inst 2007, 99:283-290.
184. Ribeiro G., Palmer M.K. Adjuvant tamoxifen for operable carcinoma of the breast: report of clinical trial by the Christie Hospital and Holt Radium Institute. Br. Med. J. (Clin. Res. Ed) 1983, 286:827-830.
185. Ribeiro G., Swindell R. The Christie Hospital tamoxifen (Nolvadex) adjuvant trial for operable breast carcinoma-7-yr results. Eur. J. Cancer Clin. Oncol 1985, 21:897-900.
186. Robinson D.R., Wu Y.M., Vats P., Su F., Lonigro R.J., Cao X., et al. Activating ESR1 mutations in hormone-resistant metastatic breast cancer. Nat. Genet 2013, 45:1446-1451.
187. Robinson S.P., Koch R., Jordan V.C. In vitro estrogenic actions in rat and human cells of hydroxylated derivatives of D16726 (zindoxifene), an agent with known antimammary cancer activity in vivo. Cancer Res 1988, 48:784-787.
188. Rossouw J.E., Anderson G.L., Prentice R.L., LaCroix A.Z., Kooperberg C., Stefanick M.L., et al. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA 2002, 288:321-333.
189. Sanchez R., Nguyen D., Rocha W., White J.H., Mader S. Diversity in the mechanisms of gene regulation by estrogen receptors. Bioessays 2002, 24:244-254.
190. Santen R.J., Brodie H., Simpson E.R., Siiteri P.K., Brodie A. History of aromatase: saga of an important biological mediator and therapeutic target. Endocr. Rev 2009, 30:343-375.
191. Schafer J.I., Liu H., Tonetti D.A., Jordan V.C. The interaction of raloxifene and the active metabolite of the antiestrogen EM-800 (SC 5705) with the human estrogen receptor. Cancer Res 1999, 59:4308-4313.
192. Schwartz J.A., Zhong L., Deighton-Collins S., Zhao C., Skafar D.F. Mutations targeted to a predicted helix in the extreme carboxyl-terminal region of the human estrogen receptor-alpha alter its response to estradiol and 4-hydroxytamoxifen. J. Biol. Chem 2002, 277:13202-13209.
193. SCTO Adjuvant tamoxifen in the management of operable breast cancer: the Scottish Trial. Lancet 1987, 2:171-175.
194. Sengupta S., Obiorah I., Maximov P.Y., Curpan R., Jordan V.C. Molecular mechanism of action of bisphenol and bisphenol A mediated by oestrogen receptor alpha in growth and apoptosis of breast cancer cells. Br. J. Pharmacol 2013, 169:167-178.
195. Shapiro S., Kelly J.P., Rosenberg L., Kaufman D.W., Helmrich S.P., Rosenshein N.B., et al. Risk of localized and widespread endometrial cancer in relation to recent and discontinued use of conjugated estrogens. N. Engl. J. Med 1985, 313:969-972.
196. Shiau A.K., Barstad D., Loria P.M., Cheng L., Kushner P.J., Agard D.A., et al. The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen. Cell 1998, 95:927-937.
197. Shike M., Doane A.S., Russo L., Cabal R., Reis-Filho J.S., Gerald W., et al. The effects of soy supplementation on gene expression in breast cancer: a randomized placebo-controlled study. J. Natl. Cancer Inst 2014, 106. 10.1093/jnci/dju189.
198. Shou J., Massarweh S., Osborne C.K., Wakeling A.E., Ali S., Weiss H., et al. Mechanisms of tamoxifen resistance: increased estrogen receptor-HER2/neu cross-talk in ER/HER2-positive breast cancer. J. Natl. Cancer Inst 2004, 96:926-935.
199. Skor M.N., Wondel E.L., Kocherginsky M., Goyal A., Hall B.A., Cai Y., et al. Glucocorticoid receptor antagonism as a novel therapy for triple-negative breast cancer. Clin. Cancer Res 2013, 19:6163-6172.
200. Sledge G.W., Mamounas E.P., Hortobagyi G.N., Burstein H.J., Goodwin P.J., Wolff A.C. Past, present, and future challenges in breast cancer treatment. J. Clin. Oncol 2014, 32:1979-1986.
201. Smith D.C., Prentice R., Thompson D.J., Herrmann W.L. Association of exogenous estrogen and endometrial carcinoma. N. Engl. J. Med 1975, 293:1164-1167.
202. Song R.X., Mor G., Naftolin F., McPherson R.A., Song J., Zhang Z., et al. Effect of long-term estrogen deprivation on apoptotic responses of breast cancer cells to 17beta-estradiol. J. Natl. Cancer Inst 2001, 93:1714-1723.
203. Speroff L. A Good Man, Gregory Goodwin Pincus: The Man, His Story, the Birth Control Pill 2009, Armica Publishing Inc., Portland, Oregon.
204. Sweeney E.E., Fan P., Jordan V.C. Mechanisms underlying differential response to estrogen-induced apoptosis in long-term estrogen-deprived breast cancer cells. Int. J. Oncol 2014, 44:1529-1538.
205. Sweeney E.E., Fan P., Jordan V.C. Molecular modulation of estrogen-induced apoptosis by synthetic progestins in hormone replacement therapy: an insight into the women's health initiative study. Cancer Res 2014, 74:7060-7068.
206. Tate A.C., Greene G.L., DeSombre E.R., Jensen E.V., Jordan V.C. Differences between estrogen- and antiestrogen-estrogen receptor complexes from human breast tumors identified with an antibody raised against the estrogen receptor. Cancer Res 1984, 44:1012-1018.
207. Tate A.C., Lieberman M.E., Jordan V.C. The inhibition of prolactin synthesis in GH3 rat pituitary tumor cells by monohydroxytamoxifen is associated with changes in the properties of the estrogen receptor. J. Steroid Biochem 1984, 20:391-395.
208. Thurlimann B., Keshaviah A., Coates A.S., Mouridsen H., Mauriac L., Forbes J.F., et al. A comparison of letrozole and tamoxifen in postmenopausal women with early breast cancer. N. Engl. J. Med 2005, 353:2747-2757.
209. Toft D., Gorski J. A receptor molecule for estrogens: isolation from the rat uterus and preliminary characterization. Proc. Natl. Acad. Sci. U.S.A. 1966, 55:1574-1581.
210. Toft D., Shyamala G., Gorski J. A receptor molecule for estrogens: studies using a cell-free system. Proc. Natl. Acad. Sci. U.S.A. 1967, 57:1740-1743.
211. Toy W., Shen Y., Won H., Green B., Sakr R.A., Will M., et al. ESR1 ligand-binding domain mutations in hormone-resistant breast cancer. Nat. Genet 2013, 45:1439-1445.
212. Umetani M., Domoto H., Gormley A.K., Yuhanna I.S., Cummins C.L., Javitt N.B., et al. 27-Hydroxycholesterol is an endogenous SERM that inhibits the cardiovascular effects of estrogen. Nat. Med 2007, 13:1185-1192.
213. Vogel V.G., Costantino J.P., Wickerham D.L., Cronin W.M., Cecchini R.S., Atkins J.N., et al. Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA 2006, 295:2727-2741.
214. Vogel V.G., Costantino J.P., Wickerham D.L., Cronin W.M., Cecchini R.S., Atkins J.N., et al. Update of the National Surgical Adjuvant Breast and Bowel Project Study of Tamoxifen and Raloxifene (STAR) P-2 Trial: preventing breast cancer. Cancer Prev. Res. (Phila.) 2010, 3:696-706.
215. Wakeling A.E., Dukes M., Bowler J. A potent specific pure antiestrogen with clinical potential. Cancer Res 1991, 51:3867-3873.
216. Walter P., Green S., Greene G., Krust A., Bornert J.M., Jeltsch J.M., et al. Cloning of the human estrogen receptor cDNA. Proc. Natl. Acad. Sci. U.S.A. 1985, 82:7889-7893.
217. Wardell S.E., Nelson E.R., Chao C.A., McDonnell D.P. Bazedoxifene exhibits antiestrogenic activity in animal models of tamoxifen-resistant breast cancer: implications for treatment of advanced disease. Clin. Cancer Res 2013, 19:2420-2431.
218. Wolf D.M., Jordan V.C. A laboratory model to explain the survival advantage observed in patients taking adjuvant tamoxifen therapy. Recent Results Cancer Res 1993, 127:23-33.
219. Wolf D.M., Jordan V.C. The estrogen receptor from a tamoxifen stimulated MCF-7 tumor variant contains a point mutation in the ligand binding domain. Breast Cancer Res. Treat 1994, 31:129-138.
220. Wu A.H., Yu M.C., Tseng C.C., Pike M.C. Epidemiology of soy exposures and breast cancer risk. Br. J. Cancer 2008, 98:9-14.
221. Wu Q., Ishikawa T., Sirianni R., Tang H., McDonald J.G., Yuhanna I.S., et al. 27-Hydroxycholesterol promotes cell-autonomous, ER-positive breast cancer growth. Cell Rep 2013, 5:637-645.
222. Yang J., Singleton D.W., Shaughnessy E.A., Khan S.A. The F-domain of estrogen receptor-alpha inhibits ligand induced receptor dimerization. Mol. Cell. Endocrinol 2008, 295:94-100.
223. Yao K., Lee E.S., Bentrem D.J., England G., Schafer J.I., O'Regan R.M., et al. Antitumor action of physiological estradiol on tamoxifen-stimulated breast tumors grown in athymic mice. Clin. Cancer Res 2000, 6:2028-2036.
224. Yu M., Bardia A., Aceto N., Bersani F., Madden M.W., Donaldson M.C., et al. Cancer therapy. Ex vivo culture of circulating breast tumor cells for individualized testing of drug susceptibility. Science 2014, 345:216-220.
225. Ziel H.K., Finkle W.D. Increased risk of endometrial carcinoma among users of conjugated estrogens. N. Engl. J. Med 1975, 293:1167-1170.