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Updated: Apr 7, 2026

Systems Biology of Metabolic Regulation by Estrogen Receptor Signaling in Breast Cancer
Published on: March 17, 2016
Effect of selective estrogen receptor modulators on metabolic homeostasis
Beibei Xu1, Dragana Lovre1, Franck Mauvais-Jarvis1
1Department of Medicine, Section of Endocrinology and Metabolism, Tulane University Health Sciences Center, School of Medicine, New Orleans, LA, USA.
Abstract:
Selective estrogen receptor modulators (SERMs) are estrogen receptor (ER) ligands that exhibit either estrogen agonistic or antagonistic activity in a tissue-specific manner. The first and second generation SERMs, tamoxifen and raloxifene, are used for treatment of ER positive breast cancer and postmenopausal osteoporosis respectively. The third-generation SERM, bazedoxifene (BZA), effectively prevents osteoporosis while blocking the estrogenic stimulation in breast and uterus. Notably, BZA combined with conjugated estrogens (CE) in a tissue-selective estrogen complex (TSEC) is a new menopausal treatment. Postmenopausal estrogen deficiency predisposes to metabolic syndrome and type 2 diabetes, and therefore the effects of SERMs and TSECs on metabolic homeostasis are gaining attention. In this article, we summarize current knowledge about the impact of SERMs on metabolic homeostasis and metabolic disorders in animal models and postmenopausal women.
Insights
Selective estrogen receptor modulators (SERMs) impact metabolic homeostasis. This review covers how SERMs and tissue-selective estrogen complexes (TSECs) affect metabolic disorders in women and animal models.
Area of Science:
- Endocrinology
- Pharmacology
- Metabolic research
Background:
- Selective estrogen receptor modulators (SERMs) are ligands targeting estrogen receptors (ER), showing tissue-specific agonist or antagonist activity.
- Tamoxifen and raloxifene (first/second-gen SERMs) treat breast cancer and osteoporosis.
- Bazedoxifene (BZA), a third-gen SERM, prevents osteoporosis while blocking estrogenic effects in breast/uterus.
Purpose of the Study:
- To summarize current knowledge on the impact of SERMs on metabolic homeostasis.
- To review the effects of SERMs and tissue-selective estrogen complexes (TSECs) on metabolic disorders.
Main Methods:
- Literature review of studies on SERMs and metabolic homeostasis.
- Analysis of data from animal models and postmenopausal women.
Main Results:
- SERMs and TSECs are investigated for their effects on metabolic homeostasis.
- Postmenopausal estrogen deficiency is linked to metabolic syndrome and type 2 diabetes.
Conclusions:
- The role of SERMs and TSECs in metabolic health is an emerging area of research.
- Understanding these effects is crucial for managing postmenopausal health and metabolic disorders.
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