Hormone replacement therapy with selective estrogen receptor modulators (SERMs) promises the highly desirable benefits of estrogen and progesterone replacement therapy, while avoiding their associated risks of breast and uterine cancer, gallbladder disease, and weight gain. In Selective Estrogen Receptor Modulators: Research and Clinical Applications, leading 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 coactivators and corepressors which modulate the estrogen receptor transcriptional activity and contribute to its crosstalk with growth factor signaling. The clinical presentations review 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 novel approach to menopause-related health issues is also provided for women with and without a previous diagnosis of localized breast cancer.
Multidisciplinary and state-of-the-art, Selective Estrogen Receptor Modulators: Research and Clinical Applications provides experimentalists and clinicians alike a comprehensive overview of the basic mechanisms of estrogen and SERMs action, as well as evidence-based guidelines for their clinical use in postmenopausal women.

Klappentext

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.

Inhalt

Basic Studies I. Molecular Mechanisms of Estrogen Receptor Function Structure and Function of the Estrogen Receptor Stefan Nilsson and Jan-Åke Gustafsson Ligand-Induced Conformational Changes in Estrogen Receptors-a and -b Elizabeth A. Allegretto Expression and Function of Estrogen Receptors-a and -b Jonathan Lindzey SERM Modulation of Gene Expression: Role of Coactivators and Corepressors Paul Webb Crosstalk Between Estrogen Receptors and Growth Factor Signaling Douglas Yee and Carol A. Lange II. Tissue-Specific Effects of Estrogens and SERMs Direct Estrogen Effects on the Cardiovascular System Munish K. Goyal and Suzanne Oparil Estrogens and the Brain: Implications for the Treatment of Postmenopausal Women Bruce S. McEwen, Phyllis M. Wise, and Stanley Birge III. Preclinical Studies Insights into the Molecular Mechanism of SERMs Through New Laboratory Models Csaba Gajdos, James Zapf, and V. Craig Jordan Third- and Fourth-Generation SERMs, Fernand Labrie Claude Labrie, Alain Bélanger, and Jacques Simard Clinical Studies IV. Organ Specific Effects of Estrogens and SERMs SERMs' Effect on the Neuroendocrine System and the Reproductive Organs Nanette F. Santoro and Peter Kovacs Epidemiology of Cardiovascular Disease in Women: Role of Estrogens Jacques E. Rossouw SERMs Effects on Cardiovascular Risk Factors and Disease Richard R. Love Estrogen and the Skeleton Michael Kleerekoper and Ashish Verma Effects of SERMs on Bone in Clinical Studies Aurelie Fontana and Pierre D. Delmas Estrogens and SERMs: Clinical Aspects of Cognition with Aging and Neurodegenerative Disorders Alan J. Lerner V. SERMs and Endocrine Dependent Tumors SERMs and Breast CancerPrevention Jenny Chang and C. Kent Osborne SERMs in Postmenopausal Women's Health Jan L. Shifren and Leo Plouffe, Jr. VI. Roles of Estrogens and SERMs in Postmenopausal Hormone Replacement Therapy Menopause Therapy: An Individualized Approach Nananda F. Col, Michele G. Cyr, and Anne W. Moulton Alternatives to Estrogen for Treatment of Menopause Richard J. Santen and JoAnn V. Pinkerton Phytoestrogens in the Context of SERMs Susan R. Davis