Danazol binding and translocation of steroid receptors
Lab / animal
OA: closed
CC0
⤵ 62 in-corpus citations
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Danazol was shown to bind and translocate steroid receptors, influencing their activity and downstream effects in cellular processes.
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Abstract
Danazol, an isoxazol derivative of ethinyl testosterone which suppresses gonadotropin levels and acts as a weak androgen, is shown by competition studies to bind rat androgen receptor (Ki 10(-8M) and progestin receptor (Ki 10(-7)M) but not estrogen receptor. Effective antigonadotropin doses to the rat in vivo translocate only androgen receptor to target cell nuclei; nuclear receptor levels remain elevated more than 6 hours. The same translocation occurs when rat uteri are incubated with danazol in vitro, showing that the action of danazol is direct and probably does not require metabolic conversion of the drug.
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References (14)
- Danazol binding to rat androgen, glucocorticoid, progesterone, and estrogen receptors: correlation with biologic activity via openalex
- Danazol Inhibits Steroidogenesis via openalex
- Effects of danazol on gonadotropin levels in castrated rhesus monkeys via openalex
- Pituitary gonadotropin responsiveness with danazol via openalex
- doi:10.1042/bj0620315 via openalex
- doi:10.1038/274276a0 via openalex
- W6716130330 via openalex
- doi:10.1016/0006-8993(79)90068-4 via openalex
- doi:10.1210/endo-101-3-920 via openalex
- doi:10.1210/endo-104-3-791 via openalex
- doi:10.1016/0022-4731(76)90095-9 via openalex
- doi:10.1016/s0015-0282(16)43869-0 via openalex
- doi:10.1016/0039-128x(77)90140-4 via openalex
- doi:10.1021/bi00724a013 via openalex
Cited by (50)
- Hormonal Therapy in Endometriosis and Adenomyosis: Danazol, Aromatase Inhibitors 2022
- Concomitant treatment of severe uterine adenomyosis in a premenopausal woman with an aromatase inhibitor and a gonadotropin-releasing hormone agonist 2007
- Hemodynamic effect of danazol therapy in women with uterine leiomyomata 2003
- A benefit-risk assessment of medical treatment for uterine leiomyomas 2002
- Behaviour of estrogen receptor, histological correlation, and clinical outcome in patients with benign breast disorders 2002
- Estudo Morfológico e Morfométrico da Mama de Ratas em Estro Permanente, Tratadas com Danazol 2001
- Novel conservative medical therapy for uterine adenomyosis with a danazol-loaded intrauterine device 2000
- Altered uterine artery blood flow impedance after danazol therapy: possible mode of action in dysfunctional uterine bleeding 1999
- Short-term treatment of uterine fibromyomas with danazol 1999
- Novel vaginal danazol ring therapy for pelvic endometriosis, in particular deeply infiltrating endometriosis 1998
- Prolonged inhibition of normal ovarian cycles in the rat and cynomolgus monkeys following a single s.c. injection of danazol 1997
- Danazol administration after gonadotrophin-releasing hormone analogue reduces rebound of uterine myomas 1997
- Leukocyte subpopulation changes in rats with autotransplanted endometrium and the effect of danazol 1995
- Pain recurrence: a quality of life issue in endometriosis 1995
- In utero virilization by danazol: Effects on adrenal steroidogenesis 1995
- Goserelin (Zoladex) versus danazol for endometriosis: the North American experience 1994
- Progesterone receptor induction by danazol in cultured cancer cells and the rat uterus 1992
- Inhibitory and stimulatory actions of danazol in rat ovarian and uterine tissues 1992
- The effects of fetal exposure to danazol 1992
- Thermoregulatory and endocrine effects of a low dose of danazol in postmenopausal women: interaction with the effect of naloxone 1991
- Tissue factors influencing growth and maintenance of endometriosis 1991
- The use of danazol as a treatment of endometriosis 1991
- Medical treatment of mild endometriosis associated with infertility 1991
- Comparison of the pharmacology of nafarelin and danazol 1990
- Studies on the mechanism of action of danazol and gestrinone (R2323) in the rat: evidence for a masked estrogen component 1989
- Danazol concentrations in human ovarian follicular fluid and their relationship to simultaneous serum concentrations 1988
- Growth inhibition by danazol in a human endometrial cancer cell line with estrogen-independent progesterone receptors 1987
- Endometriosis 1987
- Danazol binds to progesterone receptors and inhibits the growth of human endometrial cancer cells in vitro 1986
- Endocrine Therapy In Primary and Advanced Breast Cancer 1986
- Cytoplasmic and nuclear estrogen binding capacity in the rat uterus during treatment with danazol and testosterone 1986
- Inhibition of gonadotropin-releasing hormone receptors in rat anterior pituitary monolayer cell cultures by danazol 1986
- Direct biphasic effects of danazol on gonadotropin-dependent differentiation of cultured rat granulosa cells 1986
- Danazol in the treatment of endometriosis: analysis of 100 cases with a 4-year follow-up 1985
- Danazol and fetal masculinization: a warning 1985
- Cytosol estrogen and progestin receptor concentrations and 17 beta-hydroxysteroid dehydrogenase activities in the endometrium and endometriotic tissue. Effects of hormonal treatment 1984
- Short-term effects of danazol on endometrial histology 1984
- Changes in the SHBG concentration during danazol treatment 1984
- Endocrine effects of danazol in the treatment of endometriosis 1984
- Regression of endometriosis following shorter treatment with, or lower dose of danazol. Comparison of pre- and post-treatment laparoscopic findings in the Scandinavian multi-center study 1984
- The use of human skin fibroblasts to obtain potency estimates of drug binding to androgen receptors 1984
- Danazol binding to steroid receptors in human uterine endometrium 1984
- Danazol treatment of severely symptomatic fibrocystic breast disease and long-term follow-up--the Hjørring project 1984
- Progestin-like effects of danazol on rabbit uterus 1983
- Effect of danazol on gonadal steroidogenesis in patients with a complete form of testicular feminization 1982
- Influence of danazol treatment during the luteal phase on pituitary and ovarian function during the subsequent menstrual cycle 1982
- Hormonal and Surgical Management of Pelvic Endometriosis 1982
- Danazol 1982
- Estrogen and progestin receptors in endometriosis lesions: comparison with endometrial tissue 1981
- Transient adrenogenital syndrome due to exposure to danazol in utero 1981
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- last seen: 2026-05-10T10:23:40.418426+00:00
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