Selective Estrogen Receptor Modulators, 2002
Research and Clinical Applications
Contemporary Endocrinology Series

Experimental and clinical researchers from a wide range of disciplines present a wealth of fresh scientific information on the biochemistry, molecular biology, pharmacology, and clinical activity of SERMs. The basic science chapters of the book focus-with an eye to the development of the ideal SERM-on the complex mechanisms of estrogen action, including ligand-dependent conformational changes in alpha and beta, and the recruitment of co-activators and co-repressors which modulate the estrogen receptor transcriptional activity and contribute to its crosstalk with growth factor signaling. The clinical presentation reviews the data accumulated on currently available SERMs, primarily tamoxifen and raloxifene, in cancer treatment and prevention, as well as their effects on the reproductive, vascular, skeletal, and central nervous systems. A tentative approach to menopause-related health issues is also provided for women with and without a previous diagnosis of localized breast cancer.

I Molecular Mechanisms of Estrogen Receptor Function.- 1 Structure and Function of the Estrogen Receptor.- 2 Ligand-Induced Conformational Changes in Estrogen Receptors-? and -?.- 3 Expression and Function of Estrogen Receptors-? and -?.- 4 SERM Modulation of Gene Expression: Role of Coactivators and Corepressors.- 5 Crosstalk Between Estrogen Receptors and Growth Factor Signaling.- II Tissue-Specific Effects of Estrogens and SERMs.- 6 Direct Estrogen Effects on the Cardiovascular System.- 7 Estrogens and the Brain: Implications for the Treatment of Postmenopausal Women.- III Preclinical Studies.- 8 Insights into the Molecular Mechanism of SERMs Through New Laboratory Models.- 9 Third- and Fourth-Generation SERMs.- IV Organ Specific Effects of Estrogens and SERMs.- 10 SERMs’ Effect on the Neuroendocrine System and the Reproductive Organs.- 11 Epidemiology of Cardiovascular Disease in Women: Role of Estrogens.- 12 SERMs Effects on Cardiovascular Risk Factors and Disease.- 13 Estrogen and the Skeleton.- 14 Effects of SERMs on Bone in Clinical Studies.- 15 Estrogens and SERMs: Clinical Aspects of Cognition with Aging and Neurodegenerative Disorders.- V SERMs and Endocrine Dependent Tumors.- 16 SERMs and Breast Cancer Prevention.- 17 SERMs in Postmenopausal Women’s Health.- VI Roles of Estrogens and SERMs in Postmenopausal Hormone Replacement Therapy.- 18 Menopause Therapy: An Individualized Approach.- 19 Alternatives to Estrogen for Treatment of Menopause.- 20 Phytoestrogens in the Context of SERMs.

Includes supplementary material: sn.pub/extras