Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen PDF
Preview Estrogens and Antiestrogens II: Pharmacology and Clinical Application of Estrogens and Antiestrogen
Handbook of Experimental Pharmacology Volume 135/// Editorial Board G.VR. Born, London P. Cuatrecasas, Ann Arbor, MI D. Ganten, Berlin H. Herken, Berlin K. Starke, Freiburg I. Br. P. Taylor, La Jolla, CA Springer Berlin Heidelberg New York Barcelona Hong Kong London Milan Paris Singapore Tokyo Estrogens and Antiestrogens II Pharmacology and Clinical Application of Estrogens and Antiestrogens Contributors E. Anderson, A.S. Bhatnagar, H. Blode, C. Christiansen, M. Doren, M. Dowsett, K.H. Fritzemeier, R. Gallo, A.R. Genazzani, I-A. Gustafsson, Ch. Hegele-Hartung, V.W. Henderson, A. Howell, S.M. Hyder, E.V. Jensen, S.R.D. Johnston, S.K. Jonas, H.L. J lilrgensen, H. Kuhl, W. Kuhnz, G. Kuiper, S. Makela, E.F. Mammen, H.H.D. Meyer, W.R. Miller, N. Navizadeh, M. Oettel, F. Petraglia, A. Purohit, M.I Reed, L. Sahlin, G. Samsioe, B. von Schoultz, R. Sitruk- Ware, G. Soderqvist, A. Spinetti, G.M. Stancel, F.Z. Stanczyk, M. Stomati, A.E. Wakeling, M. Warner, R.O. Wharton, B. Winding, H. Zimmermann Editors M. Oettel and E. Schillinger , Springer Professor Dr. med.vet.habil. MICHAEL OETTEL Leiter Forschung und Entwicklung lenapharm GmbH & Co. KG Otto-Schott-Str. 15 0-07745 lena GERMANY Dr. rer.nat. EKKEHARD SCHILLINGER Leiter Forschung Fertilitatskontrolle und Hormontherapie Schering Aktiengesellschaft MOllerstr. 170-178 0-13342 Berlin GERMANY With 85 Figures and 62 Tables ISBN-13: 978-3-642-64261-6 e-ISBN-13: 978-3-642-60107-1 DOl: 10.1007/978-3-642-60107-1 Ubrary of Congress Cataloging·in·Publication Data Estrogens and antiestrogens I editor$, Michael Oeuel and Ekkellard Schillinger. p. cm. - (Handbook of experimental pharmacology; 135) Includes bibliographical references and index. Contents: I. Physiology and mechanisms of emogeru and antiestrogens I contributor$, s.E. Alves ... [et al.). -II. Pharmacology and clini cal application of estrogeru and antiestrogens I contributor$, E. Andenon ... [et all. ISBN 978·3-642-64261-6 I. Estrogen-Physiological effecl. 2. Estro gen-Therapeutic use. 3. Estrogen-Inhibitors-Physiolngical effect. 4. Estrogen-Inhibitors-Therapeutic usc. I. Oetlel. Michael, 1939- II. Series. [DNLM: I. Estrogens-pharmacology. 2. Estrogen AntagonislS-phannacology. 3. Estrogen Antagonists-therapeutic use. 4. Estrogens-metabolism. WI HA51L v. 135 1999 I WP 522 E807 1999) OP90S.H3 vol. 135 (OP572.E857] 615'.\ Hc21 [615'.366] DNLMJDLC for Library of Congress 99·15299 CiP This work is subject to copyright. All rights are reserved. whether the whole orpan of the material is concerned, specifically the rights of translation. reprinting. reuse of illustrations. recitation. broadcasting. reproduction on microfilm or in any other way. and storage in data banks. Duplication of this publication or parts thereof is per milled only under the provisions of the German Copyright Law of September 9, 1965, in its current version. and permission for use must always be obtained from Springer-Vedag. Violations are liable for prosecution under the German Copyright Law. (I Springer-Verlag Berlin Heidelberg 1999 Softco"cr rcprint ofthc hardcover 1st edition 1999 The use of general descriptive names. registered names. trademark$, etc. in this publication does not imply. even in the absence of a specific statement, rhat such nameli are exempt from the relevant protective laW$ and reg ulations and therefore free for general use. Product liability:The publishers cannot guarantee the accuracy of any information about dosage and applica tion contained in this book. In every individual case the user must check such infonnation by consulting the relevant literature. Cover design: dnigl1 & producriol1 GmbH. Heidelberg Typesetting: Best-sct Typesetter Ltd .. Hong Kong Production Editor: Angtlique Gcouta SPIN: 10714172 27f3020 - 5 4 3 21 0 -Printed on acid-free paper Preface For many years, Springer has been publishing an impressive series of textbooks of pharmacology which have set standards in medical science. Surprisingly, an extensive overview of the current state of the art in research on estrogens and anti estrogens was still lacking. The present two volumes on estrogens and anti estrogens provide a comprehensive review of a field of research in which remarkable progress has been made over the past few years. New insights into the mechanisms of steroid hormone action resulted in a tremendous number of pUblications from which new principles of preventive and therapeutic appli cations of estrogens and anti estrogens emerged. Although various electronic data bases provide easy access to this copious information, there was a clear necessity for a monograph-style textbook which assesses and summarizes current knowledge in this rapidly expanding field of research. It should be noted, however, that, due to this dynamic development, it is barely possible to comprehensively update every aspect of basic and clinical knowledge on estro gens and antiestrogens. Thus, the intention of the editors was to provide the reader with an overview of the "classic" and most recently explored areas of research and stimulate future interests in basic and applied endocrinology. Estrogens were among the first steroid hormones described in the scientific literature. Since they were first isolated, since the chemical, synthesic and pharmacological characterization of naturally occurring estrogens and, later on, of orally active derivatives, estrogen research has produced continu ously hallmark results in reproductive endocrinology worldwide. Develop ment of oral contraceptives consisting of estrogens and progestins has revolutionized not only fertility regulation but also society itself. The intro duction of hormone replacement therapy and an emerging awareness of its benefits has dramatically improved the quality of life of postmenopausal women. The discovery of anti estrogens and their implication for the treatment of hormone-dependent cancers has saved millions of lives. At present, an explosion of knowledge in the field of molecular biology has a tremendous influence on basic research, which addresses cellular and molecular mecha nisms of action of estrogens and anti estrogens. Estrogen research has gained substantial momentum from the discovery of different estrogen receptor iso forms (as exemplified in the chapter by Sven-Ake Gustafsson's group in Vol. I), identification of co-activators and co-repressors which interact with estro gen receptor-mediated transcription, and new insights into the physiological VI Preface importance of estrogens gathered from studies on transgenic animals. Increas ing understanding of basic mechanisms of estrogen action has paved the way for the discovery of a new class of selective ligands of the estrogen receptor, the so-called selective estrogen receptor modulators (SERMs). These com pounds may open new avenues in the prevention and treatment of dis eases. The growing importance of phytoestrogens has also been recognized. Recently, evidence has accumulated in support of the view that the biological role of estrogens is not confined to the female organism, but also has significant physiological and clinical effect on the male. The central nervous system and bone are constantly gaining importance as crucial targets of estrogen action. Finally, the issues of environmental pollution by estrogen-like compounds and metabolites and its biological consequences have become a source of increas ing concern. The contributors to this book are renowned experts in the corresponding fields of research. The editors thus focussed their effort on providing a bal anced representation of basic and clinical research from academia and the pharmaceutical industry, while deliberately abstaining from any major inter ference with the content and style of individual chapters. This might have resulted in duplication of certain aspects; however, one should consider that even research can be contemplated from different points of view. It was a rewarding endeavor to closely interact with the authors in the course of the editorial process, and we are indebted to them for their cooper ation. We extend our thanks to Doris Walker from Springer for her patience and guidance through various stages of the development of this book. Many thanks also to Hans Herken - the editor-in-chief of the whole series - for his constant interest, his moderate but inevitable pressure on the editors and finally, his patience with us. The editorial assistance of Horst Wagner is grate fully acknowledged. We also appreciate the support of many staff members at Springer, Schering, and JenaphaJ:m. M. OETIEL and E. SCHILLINGER Jena and Berlin, July 1999 List of Contributors ANDERSON, E., Royal Marsden NHS Trust, Fulham Road, London SW3 6JJ, United Kingdom BHATNAGAR,A.S., Novartis Pharma AG, K-12S.1S.16, CH-4002 Basel, Switzerland BLODE, H., Research Laboratories, Pharmakokinetik, Schering AG, D-13342 Berlin, Germany CHRISTIANSEN, c., Center for Clinical and Basic Research, Ballerup Byvej 222, DK-27S0 Ballerup, Denmark DOREN, M., King's College Hospital, Department of Family Planning, Denmark Hill, London SES 9RS, United Kingdom DOWSETT, M., Academic Department of Biochemistry, Christie Hospital NHS Trust, Manchester M20 4BX, United Kingdom FRITZEMEIER, K.H., Research Laboratories of Schering AG, Mtillerstr. 178, D-13342 Berlin, Germany GALLO, R., Department of Reproductive Medicine and Child Development, Division of Gynecology and Obstetrics, University of Pisa, Pisa, Italy GENAZZANI, Department of Reprod~ctive Medicine and Child Development, Division of Gynecology and Obstetrics, University of Pisa, Pisa, Italy GUSTAFSSON, J.-A., Department of Medical Nutrition, Karolinska Institute, NOVUM, S-14186 Huddinge, Sweden HEGELE-HARTUNG, Ch., Research Laboratories of Schering AG, Mtillerstr. 178, D-13342 Berlin, Germany VIII List of Contributors HENDERSON, V.w., Department of Neurology, University of Southern California, Los Angeles, CA 90033, USA HOWELL, A., CRC Department of Medical Oncology (University of Manchester), Christie Hospital NHS Trust, Manchester M20 4BX, United Kingdom HYDER, S.M., Department of Integrative Biology, Pharmacology and Physiology, The University of Texas Medical School at Houston, P.O. Box 20108, Houston, TX 77225, USA JENSEN, E.V., Department of Medical Nutrition, Karolinska Institutet NOVUM, S-141 86 Huddinge, Sweden JOHNSTON, S.R.D., Department of Medicine, The Royal Marsden NHS Trust, Fulham Road, London SW3 611, United Kingdom JONAS, S.K., Department of Surgery, Imperial College School of Medicine, Chelsea and Westminster Hospital, 369, Fulham Road, London SW10 9NH, United Kingdom JlZiRGENSEN, H.L., Medicon, Gydevang 24-26, P.O. Box 220, DK-3450 AllerlZid, Denmark KUHL, H., Klinik fur gynakologische Endokrinologie, Universitats Frauenklinik, Theodor-Stern-Kai 7, D-60590 Frankfurt/Main, Germany KUHNZ, w., Research Laboratories, Pharmakokinetik, Schering AG, D-13342 Berlin, Germany KUIPER, G., Department of Medical Nutrition and Department of Biosciences, Karolinska Institute, NOVUM, S-14186 Huddinge, Sweden MAKELA, S., University of Turku, Institute of Biomedicine, Department of Anatomy, Kiinamyllynkatu 10, FIN-20520 Turku, Finland MAMMEN, E.F., Department of Obstetrics and Gynecology, Wayne State University, School of Medicine, C.S. Mott Center, 275 East Hancock Ave., Detroit, MI 48201, USA Mailing address: Route 1, 1553-H2 Michibay Drive, Manistique, MI 49854, USA List of Contributors IX MEYER, H.H.D., Forschungszentrum ftir Milch und Lebensmittel Weihenstephan, Institut fUr Physiologie, Technische Universitat Mtinchen, D-85350 Freising-Weihenstephan, Germany MILLER, w.R., Breast Unit Research Group, Western General Hospital, Edinburgh EH4 2XU, United Kingdom NAVIZADEH, N., University of Southern California School of Medicine, 1240 North Mission Road, Room 1M2, Los Angeles, CA 90033, USA OETIEL, M., Jenapharm GmbH & Co. KG, Forschung und Entwicklung, Otto-Schott-Str. 15, D-07745 Jena, Germany PETRAGLIA, E, Department of Surgical Science, Chair of Obstetrics and Gynecology, University of Udine, Udine, Italy PUROHIT, A., Endocrinology and Metabolic Medicine, Imperial College of Science, Technology and Medicine, St. Mary's Hospital, London W2 INY, United Kingdom REED, M.I, Endocrinology and Metabolic Medicine, Imperial College of Science, Technology and Medicine, St. Mary's Hospital, London W2 INY, United Kingdom SAHLIN, L., Division for Reproductive Endocrinology, Department of Woman and Child Health, Karolinska Hospital L5:01, S-I71 76 Stockholm, Sweden SAMSIOE, G., Department of Obstetrics and Gynecology, Lund University Hospital, S-221 85 Lund, Sweden SCHOULTZ, B. VON, Division for Obstetrics and Gynecology, Department of Woman and Child Health, Karolinska Hospital, p.o. Box 140, S-I71 76 Stockholm, Sweden SITRUK-WARE, R., Reproductive Endocrinology, Department of Endocrinology, Saint-Antoine Hospital, Paris, France Mailing address: Exelgyn Labs, 6 rue Christophe Colomb, F-75008 Paris, France SODERQVIST, G., Department of Woman and Child Health, Division for Obstetrics and Gynecology, Karolinska Hospital, S-I71 76 Stockholm Sweden SPINETII, A., Department of Reproductive Medicine and Child Development, Division of Gynecology and Obstetrics, University of Pisa, Pisa, Italy x List of Contributors STANCEL, G.M., Department of Integrative Biology, Pharmacology and Physiology, The University of Texas Medical School at Houston, P.O. Box 207087, Houston, TX 77225, USA STANCZYK, EZ., University of Southern California School of Medicine, Department of Obstetrics and Gynecology, 1240 North Mission Road, Los Angeles, CA 90033, USA STOMATI, M., Department of Reproductive Medicine and Child Development, Division of Gynecology and Obstetrics, University of Pisa, Pisa, Italy W AKELING, A.E., Cancer and Infection Research Department, Zeneca Pharmaceuticals, Alderley Park, Macclesfield, Cheshire SKI0 4TG, United Kingdom WARNER, M., Department of Medical Nutrition and Department of Biosciences, Karolinska Institute, NOVUM, S-14186 Huddinge, Sweden WHARTON, R.Q., Department of Surgery, Imperial College School of Medicine, Chelsea and Westminster Hospital, 369, Fulham Road, London SWI0 9NH, United Kingdom WINDING, B., Center for Clinical and Basic Research, Ballerup Byvej 222, DK-2750 Ballerup, Denmark ZIMMERMANN, H., Medical Research Department, Jenapharm GmbH & Co. KG, Otto-Schott-Str. 15, D-07745 Jena, Germany
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