Selective Estrogen Receptor Modulators and Phytoestrogens: New Therapies for the Postmenopausal Woman Lorraine A. Fitzpatrick, MD Mayo Clinic Proceedings

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Selective Estrogen Receptor Modulators and Phytoestrogens: New Therapies for the Postmenopausal Woman Lorraine A. Fitzpatrick, MD Mayo Clinic Proceedings Volume 74, Issue 6, Pages 601-607 (June 1999) DOI: 10.4065/74.6.601 Copyright © 1999 Mayo Foundation for Medical Education and Research Terms and Conditions

Figure 1 An estrogen agonist or antagonist crosses the cell membrane and binds to its receptor. Estrogen receptors then dimerize, at which time they can undergo conformational changes. This dimerization may be with an identical receptor or with a different type of estrogen receptor. The dimeric receptor-ligand complex then binds to adapter proteins, which can inhibit or enhance the action of the receptor-ligand complex. This results in gene activation. Thus, there are several steps along the way in which tissue-specific effects can occur. Dimerization may occur with different types of estrogen receptors within a certain tissue. Specific tissues may contain different enhancers or inhibitors as accessory proteins and thus alter the final estrogen action. Finally, different genes may be “turned on” in specific tissues, an outcome resulting in different end points from estrogen action. Mayo Clinic Proceedings 1999 74, 601-607DOI: (10.4065/74.6.601) Copyright © 1999 Mayo Foundation for Medical Education and Research Terms and Conditions

Figure 2 Effect of raloxifene on bone mineral density at the lumbar spine, total hip, femoral neck, and total body. (From Delmas and associates.13 Copyright © 1997 Massachusetts Medical Society. All rights reserved.) Mayo Clinic Proceedings 1999 74, 601-607DOI: (10.4065/74.6.601) Copyright © 1999 Mayo Foundation for Medical Education and Research Terms and Conditions