title: Effect of selective estrogen receptor modulators on metabolic homeostasis.
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.
authors.affiliation: Department of Medicine, Section of Endocrinology and Metabolism, Tulane University Health Sciences Center, School of Medicine, New Orleans, LA, USA.
authors.forename: Beibei
authors.initials: B
authors.lastname: Xu
authors.affiliation: Department of Medicine, Section of Endocrinology and Metabolism, Tulane University Health Sciences Center, School of Medicine, New Orleans, LA, USA.
authors.forename: Dragana
authors.initials: D
authors.lastname: Lovre
authors.affiliation: Department of Medicine, Section of Endocrinology and Metabolism, Tulane University Health Sciences Center, School of Medicine, New Orleans, LA, USA. Electronic address: fmauvais@tulane.edu.
authors.forename: Franck
authors.initials: F
authors.lastname: Mauvais-Jarvis
mesh_terms: D000818:Animals; D001940:Breast / Q000378:metabolism / Q000473:pathology; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D003924:Diabetes Mellitus, Type 2 / Q000378:metabolism / Q000473:pathology; D004195:Disease Models, Animal; D004967:Estrogens / Q000378:metabolism*; D005260:Female; D006801:Humans; D007211:Indoles / Q000627:therapeutic use*; D024821:Metabolic Syndrome / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D015663:Osteoporosis, Postmenopausal / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D011960:Receptors, Estrogen / Q000378:metabolism; D014599:Uterus / Q000378:metabolism / Q000473:pathology
chemical_list: D004967:Estrogens; D007211:Indoles; D011960:Receptors, Estrogen; C447119:bazedoxifene
keywords: Bazedoxifene; Diabetes; Energy metabolism; Metabolic syndrome; Selective estrogen receptor modulators; Tissue-selective estrogen complex