Abstract
Women now live more than a third of their lives after the onset of menopause. The decline in endogenous estrogen production during this period is accompanied by functional disorders that affect quality of life. These symptoms may be relieved by menopausal hormone therapy (MHT) initially based on the administration of equine conjugated estrogens (mainly in the United States, oral route) or the natural estrogen, 17β-estradiol (in Europe, transdermal route). Estrogen receptor α (ERα), but not ERβ, mediates most of the physiological effects of estrogens. ERα belongs to the superfamily of nuclear receptors and regulates the transcription of genes via its activation functions AF1 and AF2. In addition to these classical genomic actions, estrogens can activate a subpopulation of ERα present at the cell membrane and thereby induce rapid signals. In this review, we will summarize the evolution of MHTs in last decades, as well as treatments that use various selective estrogen receptor modulators (SERMs). Next, we will describe recent advances in the understanding of the mechanisms of estrogen action, in particular the respective roles of nuclear and membrane ERα as well as the potential implications for future therapies.
Highlights
The decline in endogenous estrogen production during this period is accompanied by functional disorders that affect quality of life. These symptoms may be relieved by menopausal hormone therapy (MHT) initially based on the administration of equine conjugated estrogens or the natural estrogen, 17β-estradiol
Estrogen receptor α (ERα) belongs to the superfamily of nuclear receptors and regulates the transcription of genes via its activation functions AF1 and AF2
In addition to these classical genomic actions, estrogens can activate a subpopulation of ERα present at the cell membrane and thereby induce rapid signals
Summary
Symptômes du climatère chez les femmes non hystérectomisées Prévention de l’ostéoporose. Cancer du sein Pas d’augmentation du risque cardiovasculaire et thrombotique (voie non orale seule) dans les études de cohortes (doit être confirmée par des études randomisées). Symptômes du climatère chez les femmes hystérectomisées Prévention de l’ostéoporose. Études randomisées: Accident vasculaire cérébral Risque de thrombose veineuse Cancer du sein Accidents coronariens (>70 ans)
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