Antiestrogenic properties of keoxifene trans-4-hydroxytamoxifen, and ICI 164384, a new steroidal antiestrogen, in ZR-75-1 human breast cancer cells.
Abstract
The agonistic/antagonistic properties of two non-steroidal antiestrogens, namely trans-4-monohydroxytamoxifen (OH-TAM) and keoxifene (LY156758), and the new steroidal antiestrogen ICI164384, a 7 alpha-alkylamide derivative of estradiol (E2), were assessed by measuring their effect on the proliferation of ZR-75-1 cells, an estrogen-responsive human breast cancer cell line. While subnanomolar concentrations of both OH-TAM and LY156758 had significant estrogenic stimulatory activity on cell growth in the absence of estrogens and higher concentrations were inhibitory, ICI164384 behaved exclusively as a growth inhibitor and more potently so than the two other compounds. The three antiestrogens had similar potency to inhibit the mitogenic effect of E2 and at 300 nM, all antiproliferative effects were completely reversible by the estrogen. ICI164384 was a weaker competitor of 3H-labeled E2 or R2858 (moxestrol) uptake in intact ZR-75-1 cells in a 1-hour assay, partly because of a slower intracellular access to estrogen specific binding sites. Moreover, ICI164384 interacted in a rapidly (approximately 6 h) reversible manner with estrogen-specific binding sites, while the non-steroidal antiestrogens induced a longer-acting (greater than 24 h) down-regulation of specific [3H]R2858 uptake. The present data indicate that, among the antiestrogens studied, ICI164384 is the only compound acting as a pure antiestrogen in ZR-75-1 breast cancer cells, while LY156758 and OH-TAM behave as antiestrogens endowed with partial agonistic activity in this system.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
The antiproliferative activity of androgens in estrogen-deprived ZR-75-1 cells is more pronounced and is additive to that exerted by antiestrogens.
“Moreover, the antiproliferative activity of androgens in estrogen-deprived ZR-75-1 cells is more pronounced and is additive to that exerted by antiestrogens (208,241).”
From Endocrine and intracrine sources of androgens in women: inhibition of breast cancer and other roles of androgens and their precursor dehydroepiandrosterone (2003) · cites this paper as [241]
Cites
Yung-Chi, C., & Prusoff, W. H. (1973) · Biochemical Pharmacology · doi:10.1016/0006-2952(73)90196-2 · Cited by 12,922 · see citing works
Extension of Multiple Range Tests to Group Means with Unequal Numbers of Replications
Kramer, C. Y. (1956) · Biometrics · doi:10.2307/3001469 · Cited by 3,146 · see citing works
Berthois, Y., Katzenellenbogen, J. A., & Katzenellenbogen, B. S. (1986) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.83.8.2496 · Cited by 1,307 · see citing works
Breast Tumor Cell Lines From Pleural Effusions2
Cailleau, R., Young, R. K., Olivé, M., & Reeves, W. J. (1974) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/53.3.661 · Cited by 1,019 · see citing works
The pharmacology and clinical uses of tamoxifen
Furr, B. J. A., & Jordan, V. C. (1984) · Pharmacology & Therapeutics · doi:10.1016/0163-7258(84)90043-3 · Cited by 864 · see citing works
Estrogenic Regulation of Growth and Polypeptide Growth Factor Secretion in Human Breast Carcinoma
Dickson, R. B., & Lippman, M. E. (1987) · Endocrine Reviews · doi:10.1210/edrv-8-1-29 · Cited by 566 · see citing works
A MONOHYDROXYLATED METABOLITE OF TAMOXIFEN WITH POTENT ANTIOESTROGENIC ACTIVITY
Jordan, V. C., Collins, M. M., Rowsby, L., et al. (1977) · Journal of Endocrinology · doi:10.1677/joe.0.0750305 · Cited by 506 · see citing works
Contrasting actions of tamoxifen on endometrial and breast tumor growth in the athymic mouse.
Gottardis, M. M., Robinson, S. P., SATYASWAROOP, P. G., & Jordan, V. C. (1988) · PubMed · Cited by 422 · see citing works
Katzenellenbogen, B. S., Kendra, K. L., Norman, M. J., et al. (1987) · PubMed · Cited by 410 · see citing works
Engel, L. W., Young, N. A., Tralka, T. S., Lippman, M. E., O’Brien, S. J., & Joyce, M. J. (1978) · PubMed · Cited by 371 · see citing works
Horwitz, K. B., & McGuire, W. L. (1978) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)34379-x · Cited by 346 · see citing works
Wakeling, A. E., & Bowler, J. (1987) · Journal of Endocrinology · doi:10.1677/joe.0.112r007 · Cited by 323 · see citing works
Steroid receptor analyses of nine human breast cancer cell lines.
Horwitz, K. B., Zava, D. T., Thilagar, A. K., Jensen, E. M., & McGuire, W. L. (1978) · PubMed · Cited by 300 · see citing works
Katzenellenbogen, B. S., Norman, M. J., Eckert, R. L., Peltz, S. W., & Mangel, W. F. (1984) · PubMed · Cited by 276 · see citing works
Antagonism of estrogen action with a new benzothiophene derived antiestrogen
Black, L. J., Jones, C. D., & Falcone, J. F. (1983) · Life Sciences · doi:10.1016/0024-3205(83)90935-9 · Cited by 242 · see citing works
Dowsett, M., Goss, P. E., Powles, T., Hutchinson, G., Brodie, A. M., Jeffcoate, S. L., & Coombes, R. C. (1987) · PubMed · Cited by 238 · see citing works
Novel antioestrogens without partial agonist activity
Wakeling, A. E., & Bowler, J. (1988) · Journal of Steroid Biochemistry · doi:10.1016/0022-4731(88)90014-3 · Cited by 215 · see citing works
Eckert, R. L., & Katzenellenbogen, B. S. (1982) · PubMed · Cited by 208 · see citing works
Vignon, F., Bouton, M. M., & Rochefort, H. (1987) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(87)90819-9 · Cited by 203 · see citing works
Poulin, R., & Labrie, F. (1986) · PubMed · Cited by 200 · see citing works
Self-citationEstradiol-binding kinetics of the activated and nonactivated estrogen receptor.
Weichman, B. M., & Notides, A. C. (1977) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)38319-9 · Cited by 190 · see citing works
Bardon, S., Vignon, F., Montcourrier, P., et al. (1987) · PubMed · Cited by 173 · see citing works
Poulin, R., Baker, D., & Labrie, F. (1988) · Breast Cancer Research and Treatment · doi:10.1007/bf01805942 · Cited by 172 · see citing works
Self-citationControl of secretion and the function of C19-Δ5-steroids of the human adrenal gland
Adams, J. B. (1985) · Molecular and Cellular Endocrinology · doi:10.1016/0303-7207(85)90138-8 · Cited by 161 · see citing works
Biology and mode of action of pure antioestrogens.
Wakeling, A. E., & Bowler, J. (1988) · PubMed · doi:10.1016/0022-4731(88)90086-6 · Cited by 150 · see citing works
Uterine bioassay of tamoxifen, trioxifene and a new estrogen antagonist (LY117018) in rats and mice
Black, L. J., & Goode, R. L. (1980) · Life Sciences · doi:10.1016/0024-3205(80)90049-1 · Cited by 134 · see citing works
Reddel, R. R., & Sutherland, R. L. (1984) · European Journal of Cancer and Clinical Oncology · doi:10.1016/0277-5379(84)90062-2 · Cited by 123 · see citing works
New biospecific adsorbents for the purification of estradiol receptor.
Bucourt, R., Vignau, M., & TORELLI, V. (1978) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)34385-5 · Cited by 121 · see citing works
Rodbard, D. (1974) · Endocrinology · doi:10.1210/endo-94-5-1427 · Cited by 116 · see citing works
An Exact Correction to the “Cheng-Prusoff” Correction
Munson, P. J., & Rodbard, D. (1988) · Journal of Receptor Research · doi:10.3109/10799898809049010 · Cited by 110 · see citing works
Taylor, C. M., Blanchard, B., & Zava, D. T. (1984) · PubMed · Cited by 100 · see citing works
Mechanisms of oestrogen antagonism by nonsteroidal antioestrogens
Sutherland, R. L., & Murphy, L. C. (1982) · Molecular and Cellular Endocrinology · doi:10.1016/0303-7207(82)90165-4 · Cited by 97 · see citing works
Gulino, A., Barrera, G., Vacca, A., et al. (1986) · PubMed · Cited by 89 · see citing works
Human Breast Cancer: Biologically Active Estrogen Receptor in the Absence of Estrogen?
Zava, D. T., Chamness, G. C., Horwitz, K. B., et al. (1977) · Science · doi:10.1126/science.193182 · Cited by 85 · see citing works
Taylor, C. M., Blanchard, B., & Zava, D. T. (1984) · Journal of Steroid Biochemistry · doi:10.1016/0022-4731(84)90347-9 · Cited by 80 · see citing works
Greenberg, D. A., Carpenter, C. L., & Messing, R. O. (1987) · PubMed · Cited by 77 · see citing works
The antiproliferative effect of tamoxifen in breast cancer cells: mediation by the estrogen receptor
Bardon, S., Vignon, F., Derocq, D., et al. (1984) · Molecular and Cellular Endocrinology · doi:10.1016/0303-7207(84)90004-2 · Cited by 72 · see citing works
Raynaud, J., Martin, P., Bouton, M.-M., et al. (1978) · PubMed · Cited by 60 · see citing works
Osborne, C. K., Monaco, M. E., Kahn, C. R., et al. (1979) · PubMed · Cited by 57 · see citing works
Biological markers for breast carcinoma
Waalkes, T. P., Enterline, J. P., Shaper, J. H., Abeloff, M. D., & Ettinger, D. S. (1984) · Cancer · doi:10.1002/1097-0142(19840201)53:3+ · Cited by 49 · see citing works
Sutherland, R. L., Watts, C. K. W., & Ruenitz, P. C. (1986) · Biochemical and Biophysical Research Communications · doi:10.1016/0006-291x(86)90763-1 · Cited by 48 · see citing works
MacNab, M. W., Tallarida, R. J., & Joseph, R. R. (1984) · European Journal of Pharmacology · doi:10.1016/0014-2999(84)90493-x · Cited by 47 · see citing works
Gyling, M., & Leclercq, G. (1988) · Journal of Steroid Biochemistry · doi:10.1016/0022-4731(88)90368-8 · Cited by 41 · see citing works
Stoessel, S., & Leclercq, G. (1986) · Journal of Steroid Biochemistry · doi:10.1016/0022-4731(86)90010-5 · Cited by 40 · see citing works
Keoxifene shows pure antiestrogenic activity in pituitary gonadotrophs
Simard, J., & Labrie, F. (1985) · Molecular and Cellular Endocrinology · doi:10.1016/0303-7207(85)90131-5 · Cited by 33 · see citing works
Self-citationA novel nuclear form of estradiol receptor in MCF-7 human breast cancer cells.
Kasid, A., Strobl, J. S., Huff, K., Greene, G. L., & Lippman, M. E. (1984) · Science · doi:10.1126/science.6474170 · Cited by 32 · see citing works
Strobl, J. S., Kasid, A., Huff, K. K., et al. (1984) · Endocrinology · doi:10.1210/endo-115-3-1116 · Cited by 29 · see citing works
Fundamental research leading to improved endocrine therapy for breast cancer
Miller, W. R. (1987) · Journal of Steroid Biochemistry · doi:10.1016/0022-4731(87)90343-8 · Cited by 16 · see citing works
Sonnenschein, C., Papendorp, J. T., & Soto, A. M. (1985) · Life Sciences · doi:10.1016/0024-3205(85)90510-7 · Cited by 12 · see citing works
Biochemical and biological aspects of anti-oestrogen action
Wakeling, A. E., & Slater, S. R. (1981) · doi:10.1007/978-1-349-81345-2_12 · Cited by 12 · see citing works
Stanley, J. C. (1981) · British Journal of Anaesthesia · doi:10.1093/bja/53.2.147 · Cited by 10 · see citing works
Nelson, K., van Nagell, J. R., Gallion, H. H., et al. (1988) · PubMed · Cited by 2 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Labrie, F., Luu-The, V., Labrie, C., Bélanger, A., Simard, J., Lin, S.-X., & Pelletier, G. (2003) · Endocrine Reviews · doi:10.1210/er.2001-0031 · Cited by 544 · see citing works
Self-citationLabrie, F., Luu-The, V, Lin, S., Simard, J., Labrie, C., El-Alfy, M., Pelletier, G., & Belanger, A. (2000) · Journal of Molecular Endocrinology · doi:10.1677/jme.0.0250001 · Cited by 278 · see citing works
Self-citationDown-regulation of estrogen receptors by androgens in the ZR-75-1 human breast cancer cell line.
POULIN, R., SIMARD, J., LABRIE, C., PETITCLERC, L., DUMONT, M., LAGACÉ, L., & LABRIE, F. (1989) · Endocrinology · doi:10.1210/endo-125-1-392 · Cited by 115 · see citing works
Self-citation
- Authors
- Poulin, R., Merand, Y., Poirier, D., Levesque, C., Dufour, J.-M., & Labrie, F.
- Affiliations
- Centre hospitalier de l'Université Laval (CA)
- ORCID
- Poirier, Donald
- Venue
- Breast Cancer Research and Treatment
- Published
- 1989-10
- Volume
- 14
- Issue
- 1
- Pages
- 65-76
- ISSN
- 0167-6806 (ISSN-L)
- 1573-7217
- OpenAlex
- W1988508767
- Cited by
- 86
- References
- 52
- Citations by year
- 2017: 1 · 2016: 1 · 2012: 2
- FWCI
- 2.20
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Breast Cancer Research and Treatment (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Medical Research Council Canada
- Research England
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Breast Cancer Treatment Studies
- Physical Sciences › Environmental Science › Health, Toxicology and Mutagenesis › Effects and risks of endocrine disrupting chemicals
- Keywords
- ZR-75-1 cells, breast cancer, estrogen receptor, estrogen agonist activity, cell proliferation
- MeSH terms
- Binding, Competitive, Breast Neoplasms, Cell Division, Dexamethasone, Dose-Response Relationship, Drug, Drug Interactions, Estradiol, Estrogen Antagonists, Humans, Piperidines, Receptors, Estrogen, Dihydrotestosterone, Tamoxifen, Time Factors, Tumor Cells, Cultured, Raloxifene Hydrochloride, Polyunsaturated Alkamides
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review