A potent specific pure antiestrogen with clinical potential.
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Summary
The properties of ICI 182,780 identify this pure antiestrogen as a prime candidate with which to evaluate the potential therapeutic benefits of complete estrogen withdrawal in endocrine-responsive human breast cancer.
- Type
- article
- Published
- 1991-08-01
- Cited by
- 1,187
- References
- 42
- OpenAlex
- https://openalex.org/W1565310327
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:34242587
Keywords
Potency, Antiestrogen, In vivo, Tamoxifen, Pharmacology
References
- Effect of steroidal and nonsteroidal antiestrogens on the growth of a tamoxifen-stimulated human endometrial carcinoma (EnCa101) in athymic mice.
- Role of the two activating domains of the oestrogen receptor in the cell‐type and promoter‐context dependent agonistic activity of the anti‐oestrogen 4‐hydroxytamoxifen.
- ICI 164,384, a pure antagonist of estrogen-stimulated MCF-7 cell proliferation and invasiveness.
- Effect of estrogens and antiestrogens on growth of human breast cancer cells in athymic nude mice.
- Role of insulin-like growth factors and the type I insulin-like growth factor receptor in the estrogen-stimulated proliferation of human breast cancer cells.
- Regulation of pS2 gene expression by affinity labeling and reversibly binding estrogens and antiestrogens: comparison of effects on the native gene and on pS2-chloramphenicol acetyltransferase fusion genes transfected into MCF-7 human breast cancer cells.
- Antagonism of estrogen- and antiestrogen-induced uterine complement component C3 expression by ICI 164,384.
- Radioimmunoassay for bovine and ovine luteinizing hormone.
- Actions of oestrogens and antioestrogens on rat mammary gland development: relevance to breast cancer prevention.
- Therapeutic potential of pure antioestrogens in the treatment of breast cancer.
- Comparative studies on the effects of steroidal and nonsteroidal oestrogen antagonists on the proliferation of human breast cancer cells.
- Estrogen-responsive element of the human pS2 gene is an imperfectly palindromic sequence.
- A comparative study of the interaction of oestradiol and the steroidal pure antioestrogen, ICI 164,384, with the molybdate-stabilized oestrogen receptor.
- Estrogen Deprivation in Breast Cancer
- Tamoxifen stimulation of human breast cancer cell proliferation in vitro: a possible model for tamoxifen tumour flare.
- Novel steroidal pure antiestrogens.
- Endocrine pharmacology of antiestrogens as antitumor agents.
- Inhibition of estrogen receptor-DNA binding by the "pure" antiestrogen ICI 164,384 appears to be mediated by impaired receptor dimerization.
- Novel antioestrogens without partial agonist activity.
- Biology and mode of action of pure antioestrogens.
Cited by
- In vivo imaging in humanized mice.
- Tissue-specific actions of antioestrogens.
- Selective Estrogen Receptor Modulators: An Alternative to Hormone Replacement Therapy
- Is high-dose estrogen-induced osteogenesis in the mouse mediated by an estrogen receptor?
- Octamethylcyclotetrasiloxane exhibits estrogenic activity in mice via ERalpha.
- The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers.
- Akt-mediated phosphorylation and activation of estrogen receptor alpha is required for endometrial neoplastic transformation in Pten+/- mice.
- An overview of current and emerging SERMs.
- The role of estradiol receptor in the proliferative activity of vanadate on MCF-7 cells.
- New targeted therapies for breast cancer: A focus on tumor microenvironmental signals and chemoresistant breast cancers.
- Delay of postnatal maturation sensitizes the mouse prostate to testosterone-induced pronounced hyperplasia: protective role of estrogen receptor-beta.
- Progression of MCF-7 breast cancer cells to antiestrogen-resistant phenotype is accompanied by elevated levels of AP-1 DNA-binding activity.
- Steroidhormonrezeptor-gerichtete Therapien in der gynäkologischen Onkologie
- The duration of adjuvant tamoxifen therapy.
- Current and future roles of adjuvant endocrine therapy in the management of early carcinoma of the breast.
- Estrogens, phytoestrogens, and breast cancer.
- Fulvestrant for systemic therapy of locally advanced or metastatic breast cancer in postmenopausal women: guideline recommendations
- Improvements in tumor targeting, survivorship, and chemoprevention pioneered by tamoxifen. A personal perspective.
- Anti-estrogens induce apoptosis of multiple myeloma cells.
- Current status of estrogen receptors.
Related papers
- Tamoxifen and Norethisterone: Effects on Plasma Cholesterol and Total Body Calcium Content in the Estrogen-Deficient Rat
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- Potency and plasma protein binding of drugs in vitro—a potentially misleading pair for predicting in vivo efficacious concentrations in humans
- Modulation of rat uterine steroid hormone receptors by estrogen and antiestrogen.
- Rapid endocrine effects of tamoxifen and testolactone in prostatic carcinoma patients
- Inhibition of the uterotropic activity of estrogens and antiestrogens by the short acting antiestrogen LY117018.
- Relaxin Stimulates Uterine Edema via Activation of Estrogen Receptors: Blockade of its Effects Using ICI 182,789, a Specific Estrogen Receptor Antagonist.
- [In vivo occupation of estrogen receptors by hydroxylated metabolites of tamoxifen].
- Characterization of the ovariectomized rat model for the evaluation of estrogen effects on plasma cholesterol levels.