Pure Antiestrogens The Most Important Advance in the Endocrine Therapy of Breast Cancer since 1896? a
1996; Wiley; Volume: 784; Issue: 1 Linguagem: Inglês
10.1111/j.1749-6632.1996.tb16247.x
ISSN1749-6632
AutoresRobert I. Nicholson, Julia M.W. Gee, Sian Bryant, A Francis, R A McClelland, J M Knowlden, A. E. Wakeling, C. Kent Osborne,
Tópico(s)Monoclonal and Polyclonal Antibodies Research
ResumoAnnals of the New York Academy of SciencesVolume 784, Issue 1 p. 325-335 Pure Antiestrogens The Most Important Advance in the Endocrine Therapy of Breast Cancer since 1896?a R. I. NICHOLSON, R. I. NICHOLSON Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorJ. M. W. GEE, J. M. W. GEE Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorS. BRYANT, S. BRYANT Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorA. B. FRANCIS, A. B. FRANCIS Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorR. A. McCLELLAND, R. A. McCLELLAND Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorJ. KNOWLDEN, J. KNOWLDEN Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorA. E. WAKELING, A. E. WAKELING Zeneca Pharmaceuticals Macclesfield SK10 4TG, United KingdomSearch for more papers by this authorC. K. OSBORNE, C. K. OSBORNE Department of Medicine University of Texas Health Science Center San Antonio, Texas 78285–7884Search for more papers by this author R. I. NICHOLSON, R. I. NICHOLSON Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorJ. M. W. GEE, J. M. W. GEE Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorS. BRYANT, S. BRYANT Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorA. B. FRANCIS, A. B. FRANCIS Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorR. A. McCLELLAND, R. A. McCLELLAND Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorJ. KNOWLDEN, J. KNOWLDEN Tenovus Cancer Research Center University of Wales College of Medicine Cardiff CF4 4XX, United KingdomSearch for more papers by this authorA. E. WAKELING, A. E. WAKELING Zeneca Pharmaceuticals Macclesfield SK10 4TG, United KingdomSearch for more papers by this authorC. K. OSBORNE, C. K. OSBORNE Department of Medicine University of Texas Health Science Center San Antonio, Texas 78285–7884Search for more papers by this author First published: April 1996 https://doi.org/10.1111/j.1749-6632.1996.tb16247.xCitations: 7 a This work was financially supported by the Tenovus Organization, the Association for International Breast Cancer Research, and the National Institutes of Health (Grant Nos. CA 30251, CA 58183, and CA 54134). AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onEmailFacebookTwitterLinkedInRedditWechat References 1 Wakeling, A. E. 1993. The future of pure antiestrogens in clinical breast cancer. Breast Cancer Res. Treat. 25: 1–9. 10.1007/BF00662395 PubMedWeb of Science®Google Scholar 2 Nicholson, R. I., A. B. Francis, D. L. Manning & J. M. W. Gee. 1994. Pure antiestrogens (ICI 164384 and ICI 182780) and breast cancer: is the attainment of complete estrogen withdrawal worthwhile? Endocr. Related Cancer 1: 5–17. 10.1677/erc.0.0010005 CASWeb of Science®Google Scholar 3 Wilson, A. P. M., P. J. Weatherill, R. I. Nicholson, P. Davies & A. E. Wakeling. 1990. A comparative study of the interaction of estradiol and the steroidal pure antiestrogen, ICI 164384, with molybdate stabilized estrogen receptor. J. Steroid Biochem. 35: 421–428. 10.1016/0022-4731(90)90250-V CASPubMedWeb of Science®Google Scholar 4 Wakeling, A. E. & J. Bowler. 1987. Steroidal pure antiestrogens. J. Endocrinol. 112: R7–R10. 10.1677/joe.0.112R007 CASPubMedWeb of Science®Google Scholar 5 Nicholson, R. I., J. M. W. Gee, C. L. Eaton, D. L. Manning, R. E. Mansel, A. K. Sharma, A. Douglas-Jones, M. Price-Thomas, A. Howell, D. L. DeFriend, N. J. Bundred, E. Anderson, J. F. R. Robertson, R. W. Blamey, M. Dowsett, P. Walton & A. E. Wakeling. 1994. Pure antiestrogens in breast cancer: experimental and clinical observations. In Sex Hormones and Antihormones in Endocrine Dependent Pathology: Basic and Clinical Aspects. M. Motta & M. Serio, Eds.: 347–360. Medica/Elsevier. Amsterdam/New York . Web of Science®Google Scholar 6 DeFriend, D. L., A. Howell, R. I. Nicholson, E. Anderson, M. Dowsett, R. E. Mansel, R. W. Blamey, N. J. Bundred, J. R. Robertson, C. Saunders, M. Baum, P. Walton, F. Sutcliffe & A. E. Wakeling. 1994. Investigation of a new pure antiestrogen (ICI 182780) in women with primary breast cancer. Cancer Res. 54: 408–414. CASPubMedWeb of Science®Google Scholar 7 Howell, A., D. L. DeFriend, R. W. Blamey, J. F. Robertson & P. Walton. 1995. Response to a pure antioestrogen (ZM 182780) in tamoxifen-resistant breast cancer. Lancet 345: 29–30. 10.1016/S0140-6736(95)91156-1 CASPubMedWeb of Science®Google Scholar 8 Musgrove, E. A., A. E. Wakeling & R. L. Sutherland. 1989. Points of action of estrogen antagonists and a calmodulin antagonist within the MCF-7 human breast cancer cell cycle. Cancer Res. 49: 2398–2404. CASPubMedWeb of Science®Google Scholar 9 Wakeling, A. E., E. Newboult & S. W. Peters. 1989. Effects of antiestrogens on the proliferation of MCF-7 human breast cancer cells. J. Mol. Endocrinol. 2: 225–234. 10.1677/jme.0.0020225 CASPubMedWeb of Science®Google Scholar 10 Nicholson, R. I., K. J. Walker, N. Bouzubar, R. Wills, J. M. W. Gee, N. K. Rushmere & P. Davies. 1990. Estrogen deprivation in breast cancer: clinical, experimental, and biological aspects. Ann. N.Y. Acad. Sci. 595: 316–327. 10.1111/j.1749-6632.1990.tb34305.x CASPubMedWeb of Science®Google Scholar 11 Wiseman, L. R., A. E. Wakeling, F. E. May & B. R. Westley. 1989. Effects of the antiestrogen, ICI 164384, on estrogen-induced mRNAs in MCF-7 cells. J. Steroid Biochem. 31: 1–6. 10.1016/0022-4731(89)90349-X Web of Science®Google Scholar 12 Lykkesfeldt, A. E. & E. K. Sorensen. 1992. Effect of oestrogen and antioestrogens on cell proliferation and synthesis of secreted proteins in the human breast cancer cell line MCF-7 and a tamoxifen-resistant variant subline, AL-1. Acta Oncol. 31: 131–138. 10.3109/02841869209088892 CASPubMedWeb of Science®Google Scholar 13 Lykkesfeldt, A. E., M. W. Madsen & P. Briand. 1994. Altered expression of oestrogen-regulated genes in a tamoxifen-resistant and ICI 164384 and ICI 182780 sensitive human breast cancer cell line, MCF-7/TAMR-1. Cancer Res. 54: 1587–1595. CASPubMedWeb of Science®Google Scholar 14 Manning, D. L., R. A. McClelland, S. Bryant, J. Knowlden, J. M. W. Gee, A. B. Francis, J. F. R. Robertson, R. W. Blamey, R. L. Sutherland, C. J. Ormandy, R. E. Mansel & R. I. Nicholson. 1995. Oestrogen-regulated genes in breast cancer: role in prognosis and endocrine sensitivity. Acta Oncol. 34: 641–646. 10.3109/02841869509094041 CASPubMedWeb of Science®Google Scholar 15 Manning, D. L. & R. I. Nicholson. 1993. Isolation of pMGT1: a gene that is repressed by estrogen and increased by antiestrogens and antiprogestins. Eur. J. Cancer 29A: 759–762. 10.1016/S0959-8049(05)80362-4 CASPubMedWeb of Science®Google Scholar 16 Bates, S. E., N. E. Davidson, E. V. Valverius, C. E. Freter, R. B. Dickson, J. P. Tam, J. E. Kudlow, M. E. Lippman & D. S. Solomon. 1988. Expression of transforming growth factor alpha and its messenger ribonucleic acid in human breast cancer: its regulation by estradiol and its possible functional significance. Mol. Endocrinol. 2: 543–555. 10.1210/mend-2-6-543 CASPubMedWeb of Science®Google Scholar 17 Gee, J. M. W., J. F. R. Robertson, H. B. Hoyle, S. R. Kyme, R. A. McClelland, I. O. Ellis, R. W. Blamey & R. I. Nicholson. 1994. Immunocytochemical localization of BCL-2 protein in human breast cancer and its relationship to a series of prognostic markers and response to endocrine therapy. Int. J. Cancer 59: 619–628. 10.1002/ijc.2910590508 CASPubMedWeb of Science®Google Scholar 18 Wakeling, A. E. & J. Bowler. 1988. Novel antiestrogens without partial agonistic activity. J. Steroid Biochem. 30: 645–653. 10.1016/0022-4731(88)90014-3 Web of Science®Google Scholar 19 Wakeling, A. E., M. Dukes & J. Bowler. 1991. A potent specific pure antiestrogen with clinical potential. Cancer Res. 51: 3867–3873. CASPubMedWeb of Science®Google Scholar 20 Nicholson, R. I. 1992. Pure antioestrogens and breast cancer. In Current Directions in Cancer Chemotherapy. IBC Technical Services. London . Google Scholar 21 Gibson, M. K., L. A. Nemmers, L. A. Beckman, W. C. Beckman, V. L. Davis, S. W. Curtis & K. S. Korach. 1991. The mechanism of ICI 164384 antiestrogenicity involves rapid loss of estrogen receptor in uterine tissue. Endocrinology 129: 2000–2010. 10.1210/endo-129-4-2000 CASPubMedWeb of Science®Google Scholar 22 Dauvois, S., P. S. Danielian, R. White & M. G. Parker. 1992. Antiestrogen ICI 164384 reduces cellular estrogen receptor content by increasing its turnover. Proc. Natl. Acad. Sci. U.S.A. 89: 4037–4041. 10.1073/pnas.89.9.4037 CASPubMedWeb of Science®Google Scholar 23 Fawell, S. E., R. White, S. Hoare, M. Sydenham, M. Page & M. G. Parker. 1990. Inhibition of estrogen receptor-DNA binding by the pure antiestrogen ICI 164384 appears to be mediated by impaired receptor dimerization. Proc. Natl. Acad. Sci. U.S.A. 87: 6883–6887. 10.1073/pnas.87.17.6883 CASPubMedWeb of Science®Google Scholar 24 Eckert, R. L., A. Mullick, E. A. Rorke & B. S. Katzenellenbogen. 1984. Estrogen receptor synthesis and turnover in MCF-7 breast cancer cells measured by a density shift technique. Endocrinology 114: 629–637. 10.1210/endo-114-2-629 CASPubMedWeb of Science®Google Scholar 25 Pasqualini, J. R., B. Schatz, C. Varin & B. L. Nguyen. 1992. Recent data on estrogen sulfatases and sulfotransferases activities in human breast cancer. J. Steroid Biochem. Mol. Biol. 41: 323–329. 10.1016/0960-0760(92)90358-P CASPubMedWeb of Science®Google Scholar 26 Santner, S. J., B. Ohlsson-Wilhelm & R. J. Santen. 1993. Estrone sulfate promotes human breast cancer cell replication and nuclear uptake of estradiol in MCF-7 cell cultures. Int. J. Cancer 54: 119–124. 10.1002/ijc.2910540119 CASPubMedWeb of Science®Google Scholar 27 Howarth, N. M., A. Purohit, M. J. Reed & B. V. L. Potter. 1994. Estrone sulfamates: potential inhibitors of estrone sulfatase with therapeutic potential. J. Med. Chem. 37: 219–221. 10.1021/jm00028a002 CASPubMedWeb of Science®Google Scholar 28 Chetrite, G., C. Varin, L. Delalonde & J. R. Pasqualini. 1993. Effect of promegestone, tamoxifen, 4-hydroxytamoxifen, and ICI 164384 on the estrone sulfatase activity of human breast cancer cells. Anticancer Res. 13: 931–934. CASPubMedWeb of Science®Google Scholar 29 Stewart, A. J., M. D. Johnson, F. E. B. May & B. R. Westley. 1990. Role of insulin-like growth factors and type I insulin-like growth factor receptor in the estrogen-stimulated proliferation of human breast cancer cells. J. Biol. Chem. 265: 21172–21178. CASPubMedWeb of Science®Google Scholar 30 Stewart, A. J., B. R. Westley & F. E. B. May. 1992. Modulation of proliferative response of breast cancer cells to growth factors by oestrogen. Br. J. Cancer 66: 640–648. 10.1038/bjc.1992.330 CASPubMedWeb of Science®Google Scholar 31 Westley, B. R. & F. E. B. May. 1991. IGFs and control of cell proliferation in breast and other cancers. Rev. Endocr. Related Cancer 39: 29–34. Google Scholar 32 Ignar-Trowbridge, D. M., K. G. Nelson, M. C. Bidwell, S. W. Curtis, T. F. Washburn, J. A. McLachlan & K. S. Korach. 1992. Coupling of dual signalling pathways: epidermal growth factor action involves the estrogen receptor. Proc. Natl. Acad. Sci. U.S.A. 89: 4658–4662. 10.1073/pnas.89.10.4658 CASPubMedWeb of Science®Google Scholar 33 Wakeling, A. E. 1994. Inhibition of EGF-receptor tyrosine kinase activity by 4-aniloquinazolines. Br. J. Cancer 69: 18 (supplement XXI, abstract 6.6). Google Scholar 34 Nicholson, R. I., J. M. W. Gee, D. L. Manning, A. E. Wakeling & B. S. Katzenellenbogen. 1995. Responses to pure antiestrogens (ICI 164384, ICI 182780) in estrogen sensitive and resistant experimental and clinical breast cancer. Ann. N.Y. Acad. Sci. 761: 148–163. 10.1111/j.1749-6632.1995.tb31376.x CASPubMedWeb of Science®Google Scholar 35 Reddy, K. B., G. L. Mangold, A. K. Tandon, T. Yoneda, G. R. Mundy, A. Zilberstein & C. K. Osborne. 1992. Inhibition of breast cancer cell growth in vitro by a tyrosine kinase inhibitor. Cancer Res. 52: 3636–3641. CASPubMedWeb of Science®Google Scholar 36 Power, R. F., S. K. Mani, J. Codina, O. M. Connelly & B. W. Očmalley. 1991. Dopaminergic and ligand-independent activation of steroid hormone receptors. Science 254: 1636–1639. 10.1126/science.1749936 CASPubMedWeb of Science®Google Scholar 37 Philips, A., D. Chalbos & H. Rochefort. 1993. Estradiol increases and antiestrogens antagonize the growth factor-induced activator protein-1 activity in MCF-7 breast cancer cells without affecting c-fos and c-jun synthesis. J. Biol. Chem. 268: 14103–14108. CASPubMedWeb of Science®Google Scholar 38 Osborne, C. K., E. B. Coronado & J. P. Robinson. 1987. Human breast cancer in the athymic mouse: cytostatic effects of long-term antiestrogen therapy. Eur. J. Cancer Clin. Oncol. 23: 1189–1196. 10.1016/0277-5379(87)90154-4 CASPubMedWeb of Science®Google Scholar 39 Osborne, C. K., M. Jarman, R. McCague, E. B. Coronado, S. G. Hilsenbeck & A. E. Wakeling. 1994. The importance of tamoxifen metabolism in tamoxifen-stimulated growth. Cancer Chemother. Pharmacol. 34: 89–95. 10.1007/BF00685924 CASPubMedWeb of Science®Google Scholar 40 Gottardis, M. M. & V. C. Jordan. 1988. Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration. Cancer Res. 48: 5183–5187. CASPubMedWeb of Science®Google Scholar 41 Clarke, R., N. Brunner, B. S. Katzenellenbogen, E. W. Thompson, M. J. Norman, C. Koppi, S. Paik, M. E. Lippman & R. B. Dickson. 1989. Progression of breast cancer cells from hormone-dependent to hormone-independent growth both in vitro and in vivo. Proc. Natl. Acad. Sci. U.S.A. 86: 3649–3653. 10.1073/pnas.86.10.3649 CASPubMedWeb of Science®Google Scholar 42 Graham, M. L., J. A. Smith, P. B. Jewett & K. B. Horwitz. 1992. Heterogeneity of progesterone receptor content and remodelling by tamoxifen characterize subpopulations of cultured human breast cancer cells: analysis by quantitative dual parameter flow cytometry. Cancer Res. 52: 593–602. CASPubMedWeb of Science®Google Scholar 43 Brunner, N., B. Boysen, J. F. Kiilgaard, T. L. Frandsen, S. Jirus & R. Clarke. 1993. Resistance to 4OH-tamoxifen does not confer resistance to the steroidal antiestrogen ICI 182780, while acquired resistance to ICI 182780 results in cross-resistance to 4OH-tamoxifen. Breast Cancer Res. Treat. 27: 135 (abstract 19). Google Scholar 44 Bronzert, D. A., G. L. Greene & M. E. Lippman. 1985. Selection and characterization of breast cancer cell line resistant to the antiestrogen LY 117018. Endocrinology 117: 1409–1417. 10.1210/endo-117-4-1409 CASPubMedWeb of Science®Google Scholar 45 Clarke, R., E. W. Thompson, F. Leonessa, J. Lippman, M. McGarvey, T. L. Frandsen & N. Brunner. 1993. Hormone resistance, invasiveness, and metastatic potential in breast cancer. Breast Cancer Res. Treat. 24: 227–239. 10.1007/BF01833263 CASPubMedWeb of Science®Google Scholar 46 Gottardis, M. M., S-Y. Jiang, M-H. Jeng & V. C. Jordan. 1989. Inhibition of tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic mice by novel steroidal antiestrogens. Cancer Res. 49: 4090–4093. CASPubMedWeb of Science®Google Scholar 47 Osborne, C. K., E. B. Coronado-Heinsohn, B. L. McCue, A. E. Wakeling & R. I. Nicholson. 1995. Comparison of the effects of a steroidal antiestrogen with those of tamoxifen in a model of human breast cancer. J. Natl. Cancer Inst. In press. 10.1093/jnci/87.10.746 PubMedWeb of Science®Google Scholar 48 Reece, J. C. & B. S. Katzenellenbogen. 1992. Examination of the DNA-binding ability of ER in whole cells: implications for hormone-independent transactivation and the actions of antiestrogens. Mol. Cell. Biol. 12: 4531–4538. PubMedWeb of Science®Google Scholar 49 Katzenellenbogen, B. S., K. L. Kendra, M. J. Norman & Y. Berrthois. 1987. Proliferation, hormonal responsiveness, and estrogen receptor content of MCF-7 human breast cancer cells grown in the short-term and long-term absence of estrogens. Cancer Res. 47: 4355–4360. CASPubMedWeb of Science®Google Scholar 50 Cho, H., P. A. Ng & B. S. Katzenellenbogen. 1991. Differential regulation of gene expression by estrogen in estrogen growth-independent and -dependent MCF-7 human breast cancer cell sublines. Mol. Endocrinol. 5: 1323–1330. 10.1210/mend-5-9-1323 CASPubMedWeb of Science®Google Scholar 51 Nicholson, R. I., A. B. Francis, J. M. W. Gee, D. L. Manning, A. E. Wakeling & B. S. Katzenellenbogen. 1995. Observations arising from the use of pure antiestrogens on estrogen-responsive (MCF-7) and estrogen growth-independent (K3) human breast cancer cells. Endocr. Related Cancer 2: 115–121. 10.1677/erc.0.0020115 CASWeb of Science®Google Scholar 52 Nunez, A., M. Berry, J. L. Imler & P. Chambon. 1989. The 5č-flanking region of the pS2 gene contains a complex enhancer region responsive to estrogens, epidermal growth factor, a tumor promoter (TPA), the c-Ha-ras oncoprotein, and the c-jun protein. EMBO J. 8: 823–829. 10.1002/j.1460-2075.1989.tb03443.x CASPubMedWeb of Science®Google Scholar 53 Nicholson, R. I., R. A. McClelland, J. M. W. Gee, D. L. Manning, P. Cannon, J. F. R. Robertson, I. O. Ellis & R. W. Blamey. 1994. Epidermal growth factor expression in breast cancer: association with responses to endocrine therapy. Breast Cancer Res. Treat. 29: 117–125. 10.1007/BF00666187 CASPubMedWeb of Science®Google Scholar 54 Davidson, N. E., E. P. Gelmann, M. E. Lippman & R. B. Dickson. 1987. Epidermal growth factor receptor gene expression in estrogen receptor positive and negative human breast cancer cell lines. Mol. Endocrinol. 1: 216–223. 10.1210/mend-1-3-216 CASPubMedWeb of Science®Google Scholar 55 Howell, A., D. J. Dodwell, I. Laidlaw, H. Anderson & E. Anderson. 1990. Tamoxifen as an agonist for metastatic breast cancer. In Endocrine Therapy of Breast Cancer IV. A. Goldhirsch, Ed.: 49–58. Springer-Verlag. Berlin/New York . 10.1007/978-3-642-75948-2_7 Web of Science®Google Scholar 56 Howell, A., D. J. Dodwell, H. Anderson & J. Redford. 1992. Response after withdrawal of tamoxifen and progestins in advanced breast cancer. Ann. Oncol. 3: 611–617. 10.1093/oxfordjournals.annonc.a058286 CASPubMedWeb of Science®Google Scholar 57 Wilson, A. J. 1983. Response in breast cancer to a second hormonal therapy. Rev. Endocr. Related Cancer 14: 5–11. Google Scholar 58 Vogel, C. L., I. Shemano, J. Schoenfelder, P. A. Gams & M. R. Green. 1993. Multicenter phase II efficacy trial of toremifene in tamoxifen-refractory patients with advanced breast cancer. J. Clin. Oncol. 11: 345–350. 10.1200/JCO.1993.11.2.345 PubMedWeb of Science®Google Scholar 59 Nicholson, R. I. 1993. Recent advances in the antihormonal therapy of breast cancer. Curr. Opin. Invest. Drugs 2: 1259–1268. Google Scholar 60 Nicholson, R. I., D. L. Manning & J. M. W. Gee. 1993. New antihormonal approaches to breast cancer therapy. Drugs Today 29: 363–372. Google Scholar Citing Literature Volume784, Issue1Basis for Cancer ManagementApril 1996Pages 325-335 ReferencesRelatedInformation
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