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.

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5: Pharmacology of Estrogens and Antiestrogens.- In Vitro and In Vivo Models to Characterise Estrogens and Antiestrogens.- A. General Aspects.- I. Physiological Targets of Estrogens.- II. ER Ligands.- III. The Receptors - Mediators of Hormone Action, Targets for Antihormones and Modulators of Gene Expression.- B. In Vitro Methods to Characterise Estrogens and Antiestrogens.- I. Receptor-Binding Assay.- 1. Principle.- 2. Binding of Estrogens and Antiestrogens to Insect- Cell-Produced Human ERa (hERa).- a) Preparation of ER-Containing Cytosol..- b) Competition Experiment.- c) Results.- II. Ligand Effects on DNA Binding of the ER.- III. Transactivation Assays for Detection of Estrogenic and Antiestrogenic Activity.- 1. Principle.- 2. Transactivation Assay with the Vitellogenin A2-ERE-tk-CAT Reporter Gene in HeLa Cells.- a) Comparative Study of the Agonistic Potency of Four Selected Estrogens.- b) Comparative Study of the Antagonistic Potency of Selected Antiestrogens.- 3. Transactivation Assay with MVLN Cell.- 4. Comparative Study of the Transactivational Activity of ERa and ERf3.- 5. Transactivation Assay with an rPR-ERE-tk-CAT Reporter Gene.- IV. Transactivation Assay in Yeast as a Model System to Characterise Estrogenic Compounds.- 1. Principle.- Determination of the Agonistic Activity of Selected Phyto- and Mycoestrogens by Transactivation Assay in Yeast..- The Yeast Strain.- Vector Plasmids.- Recombinant Yeast Strains.- Transactivation Assay.- V. Reporter Assays Based on "Non-Classical" Mechanisms of Gene Activation by the ER.- 1. ER Activation of Genes Through AP-1.- 2. TGF-fJ3 Induction Through a Non-Classical ERE.- a) Study of Raloxifen and ZM182,780 in the TGF-f?Ass.- 3. Repression of the IL-6 Gene Expression by the ER.- VI. Estrogen Effects on Expression of Endogenous Genes in Diverse Cell Lines.- 1. Alkaline Phosphatase and PR Measurement in Ishikawa Endometrial Carcinoma Cells.- 2. The Endometrial Adenocarcinoma Cell Line RUCA-I as an In Vitro/In VivoTumor Model.- 3. Cathepsin D, PS2 and PR Induction in Mammary Cell Lines by Estrogens.- a) Estrogen Effects on the PR Level in MCF-7 Cell.- b) Estrogen Effects on the Cathepsin D and pS2 mRNA Levels and on the PR Protein Level in MCF-7 Cells.- 4. Estrogen Regulation of Prolactin Expression in Pituitary Cell.- 5. Estrogen-Regulated Genes in Liver Hepatoma Cells.- 6. Induction of ERs and Vitellogenin Synthesis in Fish Liver Cells.- VII. Ligand-Induced ER Stabilisation or Destabilisation.- 1. Comparative Study of the Effects of Different Antiestrogens on the ER Level in T47-D Cells.- VIII. Effects of ER Ligands on the Proliferation of ER-Expressing Breast Cancer and Endometrial Cell Lines.- 1. Inhibition of Estrogen-Stimulated Growth of MCF-7 Mammary Carcinoma Cells by Antiestrogens.- Experimental Design.- IX. Antioxidative Activity.- 1. Protection from Amyloid-Induced Neurotoxicity and Prevention of Glutamate-Induced Cell Death in Nerve Cell.- 2. Attenuation of Lipid Peroxidation in Synaptosomal Membranes.- 3. Fe(II) Autoxidation and Fe(III) Reduction Assays.- 4. Oxidation of Low-Density Lipoprotein Cholesterol.- C. In Vivo Test Systems to Characterise Estrogens and Antiestrogens.- I. Allen-Doisy Assay.- 1. Principle.- 2. Study Design.- 3. Scoring Criteria.- 4. Evaluation and Discussion.- II. Vaginal Mitosis and Epithelial Thickness.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- III. Vaginal Tetrazolium Reduction.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- IV. Vaginal Opening.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- V. Vaginotrophic Response.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- VI. Measurement of Sialic Acid.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- VII. Uterine Fluid Inhibition (Astwood Bioassay.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- VIII. Uterine Growth Tes.- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- IX. Regulation of Steroid Hormone Receptors, Proliferation, Differentiation and Protein Expression in the Rodent Uterus.- 1. Principle.- Steroid Hormone Receptors.- Proliferation.- Protooncogenes.- Luminal Epithelial Cell Height.- Uterine Glycogen Deposition.- Peroxidase Activity.- Complement Component C3.- 2. Study Design.- Steroid Hormone Receptors.- Proliferation.- Protooncogenes.- Luminal Epithelial Cell Height.- Uterine Glycogen Deposition.- Peroxidase Activity.- Complement Component C3.- 3. Evaluation and Discussion.- Steroid Hormone Receptors.- Proliferation.- Protooncogenes.- Luminal Epithelial Cell Height.- Uterine Glycogen Deposition.- Peroxidase Activity.- Complement Component C3.- X. Withdrawal Bleeding (Primates).- 1. Principle.- 2. Study Design.- 3. Evaluation and Discussion.- XI. Imaging of the Primate Uterus.- 1. Principle.- 2. Experimental Design.- MRI Evaluation.- Ultrasound Evaluation.- 3. Evaluation and Discussion.- XII. Pituitary Blockade.- Gonadal Growth Methods.- Gonadotropin Methods.- Ovulatory Methods.- D. Transgenic Animals.- I. ERKO Mouse.- Uterus.- Ovary.- Testis.- Mammary Gland.- Behaviour.- II.PR Mutant Mouse.- Uterus.- Ovary.- Mammary Gland.- Behaviour.- References.- Estrogen Receptor ? in the Pharmacology of Estrogens and Antiestrogens.- A. Introduction.- B. Basic Similarities Between ER? and ER?.- C. ER? Isoforms.- D. Role of Ligands in the Tissue-Specific Action of ER?.- E. Tissue Distribution of ER? mRNA and Protein.- F. Multiple Mechanisms of Transcriptional Activation and Repression by ERs.- G. What is the Phenotype of ER? Knockout Mice.- References.- Interrelationship of Estrogens with other Hormones or Endocrine Systems.- A. Introduction.- B. Thyroid Hormone Effects on Estrogen Levels.- C. Estrogen Effects on Thyroid Function.- D. Estrogen Effects on the Gastrointestinal System.- E. Estrogen Effects on the Pancreas.- F. Estrogen Effects on the Parathyroid.- G. Conclusion.- Reference.- Mammary Gland.- A. Pharmacological and Physiological Effects of Estrogens in the Mammary Gland.- I. Introduction.- II. Hormone Action on the Development of the Mammary Gland.- 1. Pregnancy.- III. Proliferation.- 1. Progestogen Effects are Complex.- IV. Apoptosis.- V. Estrogen Action During the Normal Menstrual Cycle.- 1. Estrogen and Progesteron…