The steroidal antiestrogen ICI 182,780 is an inhibitor of cellular aromatase activity

Journal of Steroid Biochemistry and Molecular Biology

Volumn 67, Issue 4, 1998, Pages 293-304

  Long, Brian J ^a   Tilghman, Syreeta L ^a   Yue, Wei ^a   Thiantanawat, Apinya ^a   Grigoryev, Dmitry N ^a   Brodie, Angela M H ^a  

^a UNIVERSITY OF MARYLAND SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANASTROZOLE; AROMATASE; DEXAMETHASONE; ESTROGEN; FORMESTANE; FULVESTRANT; LETROZOLE; TAMOXIFEN;

ARTICLE; BREAST CARCINOMA; CANCER CELL CULTURE; CANCER RESISTANCE; CONTROLLED STUDY; DRUG MECHANISM; DRUG POTENCY; ENZYME SUBSTRATE; ESTROGEN RELEASE; FIBROBLAST; HUMAN; HUMAN CELL; HUMAN TISSUE; PLACENTA;

ANDROSTENEDIONE; AROMATASE; AROMATASE INHIBITORS; BASE SEQUENCE; BREAST NEOPLASMS; CELL DIVISION; CELLS, CULTURED; CHORIOCARCINOMA; DNA PRIMERS; ENZYME INHIBITORS; ESTRADIOL; ESTROGEN ANTAGONISTS; FEMALE; FIBROBLASTS; HUMANS; MICROSOMES; NITRILES; PLACENTA; RNA, MESSENGER; TRIAZOLES; TUMOR CELLS, CULTURED;

MINK CELL FOCUS-FORMING VIRUS;

EID: 0032213907     PISSN: 09600760     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-0760(98)00122-8     Document Type: Article

References (36)

1. 1. Litherland S. and Jackson I. M., Antiestrogens in the management of hormone-dependent breast cancer. Cancer Treat. Rev. 15 (1988) 183-194.
2. 2. Early Breast Cancer Trialists' Collaborative Group Systemic treatment of early breast cancer by hormonal, cytotoxic or immune therapy: 133 randomized trials involving 31000 recurrences and 24000 deaths among 75000 women. Lancet 339 (1-15) (1992) 71-85.
3. 3. Berry M., Metzger D. and Chambon P., Role of the two activating domains on the oestrogen receptor in the cell-type and promoter-context dependent agonist activity of the anti-oestrogen 4-hydroxytamoxifen. EMBO J. 9 (1990) 2811-2818.
4. 4. Furr B. J. and Jordan V. C., The pharmacology and clinical uses of tamoxifen. Pharmacol. Ther. 25 (1984) 127-205.
5. 5. Leonessa F., Boulay V., Wright A., Thompson E. W., Brünner N. and Clarke R., The biology of breast tumor progression: acquisition of hormone-independence and resistance to cytotoxic drugs. Acta Oncol. 31 (1992) 115-123.
6. 6. Fisher B., Constantino J. P., Redmond C. K., Fisher E. R., Wickerham D. L. and Cronin W. M., 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. 86 (1994) 527-537.
7. 7. Assikis V. J. and Jordan V. C., Risks and benefits of tamoxifen therapy. Oncology 11 (1997) 21-33.
8. 8. Wakeling A. E., Dukes M. and Bowler J., A potent specific pure anti-oestrogen with clinical potential. Cancer Res. 51 (1991) 3867-3873.
9. 9. Osborne C. K., Coronado-Heinsohn E. B., Hilsenbeck S. G., McCue B. L., Wakeling A. E., McClelland R. A., Manning D. L. and Nicholson R. I., Comparison of the effects of a pure steroidal antiestrogen with those of tamoxifen in a model of human breast cancer. J. Natl. Cancer Inst. 87 (1995) 747-750.
10. 10. Brünner N., Fransden T. L., Holst-Hansen C., Bei M., Thompson E. W., Wakeling A. E., Lippman M. E. and Clarke R., MCF7/LCC2: A 4-hydroxytamoxifen resistant human breast cancer variant that retains sensitivity to the steroidal antiestrogen ICI 182,780. Cancer Res. 53 (1993) 3229-3232.
11. 11. Brünner N., Boysen B., Jirus S., Skaar T. C., Holst-Hansen C., Lippman J., Fransden T., Spang-Thomsen M., Fuqua S. A. W. and Clarke R., MCF7/LCC9: An antiestrogen-resistant variant in which acquired resistance to the steroidal antiestrogen ICI 182,780 confers an early cross-resistance to the nonsteroidal antiestrogen tamoxifen. Cancer Res. 57 (1997) 3486-3493.
12. 12. Kumar V. and Chambon P., The estrogen receptor binds tightly to its response element as a ligand-induced homodimer. Cell 55 (1988) 145-156.
13. 13. Defriend D. J., Howell A., Nicholson R. I., Anderson E., Dowsett M., Mansel R. E., Blamey R. W., Bundred N. J., Robertson R. F., Saunders C., Baum M., Walton P., Sutcliffe F. and Wakeling A. E., Investigation of a new pure antiestrogen (ICI 182,780) in women with primary breast cancer. Cancer Res. 54 (1994) 408-414.
14. 14. Howell A., DeFriend D., Robertson J., Blamey R. and Walton P., Response to a specific antiestrogen (ICI 182,780) in tamoxifen-resistant breast cancer. Lancet 345 (1995) 29-30.
15. 15. Howell A., DeFriend D. J., Robertson J. F. R., Blamey R. W., Anderson L., Anderson E., Sutcliff F. A. and Walton P., Pharmacokinetics, pharmacological and anti-tumour effects of the specific anti-oestrogen ICI 182,780 in women with advanced breast cancer. British J. Cancer 74 (1996) 300-308.
16. 16. Schacter L. P., Rozencweig M., Canetta R., Kelley S., Nicaise C. and Smaldone L., Overview of hormonal therapy in advanced breast cancer. Sem. Oncol. 17 (1990) 38-46.
17. 17. Coombes R. C., Goss P. C., Dowsett M., Gazet J. C. and Brodie A. M. H., 4-hydroxyandrostenedione treatment of postmenopausal patients with advanced breast cancer. Lancet 2 (1984) 1237-1239.
18. 18. Dowsett M. and Coombes R. C., Second generation aromatase inhibitor - 4-hydroxyandrostenedione. Breast Cancer Res. Treat. 30 (1994) 81-87.
19. 19. Brodie A. M. H. and Njar C. V., Aromatase inhibitors and breast cancer. Semin. Oncol. 23 (1996) 10-20.
20. 20. Zhou D., Pompon D. and Chen S., Stable expression of human aromatase complementary DNA in mammalian cells: A useful system for aromatase inhibitor screening. Cancer Res. 50 (1990) 6949-6954.
21. 21. Yue W. and Brodie A. M. H., Mechanisms of action of aromatase inhibitors 4-hydroxyandrostenedione, fadrazole, and aminoglutethimide on aromatase in JEG-3 cell culture. J. Steroid Biochem. Molec. Biol. 63 (1997) 317-328.
22. 22. Brodie A. M. H., Schwarzel W. C., Shaikh A. A. and Brodie H. J., The effect of an aromatase inhibitor, 4-hydroxy-4-androstene-3,17-dione, on estrogen-dependent processes in reproduction and breast cancer. Endocrinology 100 (1977) 1684-1695.
23. 23. Lu Q., Nakamura J., Savinov A., Yue W., Weisz J., Dabbs D. J., Wolz G. and Brodie A., Expression of aromatase protein and messenger ribonucleic acid in tumor epithelial cells and evidence of functional significance of locally produced estrogen in human breast cancers. Endocrinology 137 (1996) 3061-3068.
24. 24. Koos R. D., Banks P. K., Inkster S. E., Yue W. and Brodie A. M. H., Detection of aromatase and keratinocyte growth factor expression in breast tumors using reverse transcription-polymerase chain reaction. J. Steroid Biochem. Molec. Biol. 45 (1993) 217-225.
25. 25. Asahara T., Murohara T., Sullivan A., Silver M., van der Zee R., Li T., Witzenbichler B., Schatteman G. and Isner J. M., Isolation of putative progenitor endothelial cells for angiogenesis. Science 275 (1997) 964-967.
26. 26. Mendelson C. R., Cleland W. H., Smith M. E. and Simpson E. R., Regulation of aromatase activity of stromal cells derived from human adipose tissue. Endocrinology 111 (1982) 1077-1084.
27. 27. Miller W. R. and Mullen P., Factors influencing aromatase activity in the breast. J. Steroid Biochem. Molec. Biol. 44 (1993) 597-604.
28. 28. Busch H., Adducts and tamoxifen. Semin Oncol. 24 (1997) S1-S98.
29. 29. Li D., Dragan Y., Jordan V. C., Wang M. and Pitot H. C., Effects of chronic administration of tamoxifen and toremifene on DNA adducts in the rat liver, kidney and uterus. Cancer Res. 57 (1997) 1438-1441.
30. 30. Dauvois S., Danielian P. S., White R. and Parker M. G., Antiestrogen ICI 164,384 reduces cellular estrogen content by increasing its turnover. Proc. Natl. Acad. Sci. U.S.A. 89 (1992) 4037-4041.
31. 31. Thomas E. J., Walton P. L., Thomas N. M. and Dowsett M., The effects of ICI 182,780, a pure anti-oestrogen, on the hypothalamic-pituitary-gonadal axis and on endometrial proliferation in pre-menopausal women. Human Reprod. 9 (1994) 1991-1996.
32. 32. Brueggemeier R. W., Li P.-K., Snider C. E., Darby M. V. and Katlic N. E., 7α-substituted androstenediones as effective in vitro and in vivo inhibitors of aromatase. Steroids 50 (1987) 163-178.
33. 33. Brueggemeier R. W., O'Reilly J. M., Lovely C. J., Ward P. J., Quinn A. L., Baker D., Darby M. V., Gu X.-J. and Gilbert N. E., Biochemistry and pharmacology of 7α-substituted androstenediones as aromatase inhibitors. J. Steroid Biochem. Molec. Biol. 61 (1997) 247-254.
34. 34. Brueggemeier R. W., Li P. K., Chen H. H., Moh P. P. and Katlic N. E., Biochemical pharmacology of new 7-substituted androstenediones as inhibitors of aromatase. J. Steroid Biochem. Molec. Biol. 37 (1990) 379-385.
35. 35. Brodie A. M. H., Hendrickson J. R., Tsai-Morris C. H., Garrett W. M., Marcotte P. A. and Robinson C. H., Inactivation of aromatase in vitro by 4-OHA and 4-acetoxyandrostenedione and sustained effects in vivo. Steroids 38 (1981) 693-702.
36. 36. Yue W., Wang J.-P., Hamilton C. J., Demers L. M. and Santen R. J., In situ arornatization enhances breast tumor estradiol levels and cellular proliferation. Cancer Res. 58 (1998) 927-932.