Skip to Main content Skip to Navigation
Journal articles

Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites.

Abstract : This work was undertaken (i) to study deeply the estrogen, androgen and progestative activities of tibolone and its metabolites (ii) to determine whether tibolone and its metabolites present glucocorticoid or mineralocorticoid activity. For this purpose, we used human cell lines bearing a luciferase gene with a responsive element under the control of human estrogen receptor alpha (ERalpha) or estrogen receptor beta (ERbeta) or androgen receptor (AR) or chimeric Gal4 fusion with progesterone receptor (PR), glucocorticoid receptor (GR) or mineralocorticoid receptor (MR). The major tibolone metabolites, the two hydroxymetabolites, bind and activate ER with a preference for ERalpha. Tibolone and the Delta(4)-tibolone are agonists for AR and PR and surprisingly 3alpha- and 3beta-OH-tibolone are antagonists for them. Moreover we showed for the first time that tibolone and its primary metabolites are GR and MR antagonists with a stronger affinity for MR than for GR. In conclusion, tibolone by these actions on different receptors and by this capacity to transform in different metabolites, has more complex effects than initially supposed.
Complete list of metadatas

https://www.hal.inserm.fr/inserm-00396319
Contributor : Yves Le Ster <>
Submitted on : Wednesday, June 17, 2009 - 3:50:28 PM
Last modification on : Tuesday, November 24, 2020 - 9:12:03 AM
Long-term archiving on: : Monday, October 15, 2012 - 12:31:51 PM

Identifiers

Collections

Citation

Aurélie Escande, Nadège Servant, Fanja Rabenoelina, Gilles Auzou, Helenius Kloosterboer, et al.. Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites.. Journal of Steroid Biochemistry and Molecular Biology, Elsevier, 2009, 116 (1-2), pp.8-14. ⟨10.1016/j.jsbmb.2009.03.008⟩. ⟨inserm-00396319⟩

Share

Metrics

Record views

451

Files downloads

1001