Inhibition of steroid sulfatase activity by danazol
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Danazol at therapeutic concentrations potently inhibits human steroid sulfatase activity in liver and breast tumor preparations, impacting estrogen formation from estrone sulfate.
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Abstract
The hydrolysis of dehydroepiandrosterone sulfate (DHAS) by human liver cells in culture and the hydrolysis of and formation of estradiol-17 beta (E2) from estrone sulfate (E1S) by human breast tumor preparations in vitro were studies in the presence and absence of danazol. In the latter tissue the effects of medroxyprogesterone acetate (MPA), trilostane, aminoglutethimide (AG) and tamoxifen were tested for comparison. Danazol at concentrations of 10(-6) - 1.4 X 10(-4) M strongly inhibited the hydrolysis of DHAS as well as the hydrolysis of and formation of E2 from E1S. With the exception of a slight inhibitory effect of trilostane upon E1S hydrolysis, the other four drugs did not inhibit the metabolism of E1S. Danazol, at concentrations corresponding to those occurring in vivo during therapy, is a potent inhibitor of steroid sulfatase activity. This may be one of the ways in which the drug affects peripheral and target tissue levels of steroid hormones.
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References (23)
- Peripheral androgen levels in danazol-treated premenopausal women via openalex
- Pharmacology and Pharmacokinetics of Danazol via openalex
- doi:10.1007/978-3-642-49793-3_5 via openalex
- doi:10.1007/978-3-642-95177-0_5 via openalex
- doi:10.3109/00016348309154229 via openalex
- W1941075922 via openalex
- doi:10.1016/0022-4731(75)90148-x via openalex
- W6667823344 via openalex
- doi:10.1016/0014-2964(80)90292-3 via openalex
- doi:10.1016/0005-2744(72)90239-2 via openalex
- doi:10.1016/s0021-9258(19)43661-2 via openalex
- doi:10.1007/978-3-642-95177-0_6 via openalex
- doi:10.1016/0022-4731(80)90050-3 via openalex
- doi:10.1530/acta.0.052s0008 via openalex
- doi:10.1016/0022-4731(74)90075-2 via openalex
- doi:10.1016/0003-9861(76)90339-8 via openalex
- doi:10.1016/s0300-595x(81)80041-2 via openalex
- doi:10.1016/0039-128x(73)90134-7 via openalex
- doi:10.3181/00379727-87-21406 via openalex
- doi:10.1210/endo-93-1-172 via openalex
- doi:10.1021/bi00830a007 via openalex
- doi:10.1007/978-3-642-49793-3_6 via openalex
- doi:10.1210/jcem-53-1-58 via openalex
Cited by (14)
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- Inhibition of steroid sulphatase activity in endometriotic implants by 667 COUMATE: a potential new therapy 2007
- Expression und Regulation von Enzymen des Östrogenmetabolismus in humanen Endometriumläsionen kultiviert in der Nacktmaus 2007
- [<sup>3</sup>H]Dexamethasone Binding Activity in Liver Microsomes is Modulated Differently by 17 α‐Alkylated Androgens and Testosterone<i>in vivo</i> 1995
- Postmenopausal endometrial hyperplasia: role of danazol therapy 1994
- Adrenal Steroids in Serum during Danazol Therapy, Taking into Account Cross-Reactions between Danazol Metabolites and Serum Androgens. 1993
- Action of danazol on the conversion of estrone sulfate to estradiol and on the sulfatase activity in the MCF-7, T-47D and MDA-MB-231 human mammary cancer cells 1993
- Inhibitory and stimulatory actions of danazol in rat ovarian and uterine tissues 1992
- Inhibition of oestrogen synthesis in postmenopausal women with breast cancer 1992
- Oestrogen sulphatase activity in hormone‐dependent and hormone‐independent breast‐cancer cells: Modulation by steroidal and non‐steroidal therapeutic agents 1992
- Endometrial Effects of Danazol in Perimenopausal Abnormal Bleeding 1991
- Danazol concentrations in human ovarian follicular fluid and their relationship to simultaneous serum concentrations 1988
- Endocrine consequences of danazol treatment in menorrhagia 1986
- Changes in the shbg concentration during danazol treatment 1984
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