Receptors and Hormone Action

Receptors and Hormone Action

Volume II

1st Edition - January 1, 1978

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  • Editors: Bert W. O'Malley, Lutz Birnbaumer
  • eBook ISBN: 9781483262710

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Receptors and Hormone Action, Volume II, is part of a multivolume series that summarizes advances in the field of hormone action. The articles contained in these books are oriented toward a description of basic methodologies and model systems used in the exploration of the molecular bases of hormone action, and are aimed at a broad spectrum of readers including those who have not yet worked in the field as well as those who have considerable expertise in one or another aspect of hormone action. The book opens with a chapter on the relationship between steroid hormone-receptor binding and biologic response. This is followed by separate chapters on conformational forms of the estrogen receptor; the relationship of early responses of the cell to estrogen to DNA synthesis; the role of receptors in the anabolic action of androgens; and biology of progesterone receptors. Subsequent chapters deal with the molecular structure and analysis of progesterone receptors; the regulation of gene expression by glucocorticoid hormones; studies of the aldosterone receptor in the adrenalectomized rat kidney; and existence of gonadal steroid receptors in brain and pituitary tissue.

Table of Contents

  • List of Contributors


    1 The Biology and Pharmacology of Estrogen Receptor Binding: Relationship to Uterine Growth

    I. Introduction

    II. Relationship between Receptor Binding and Uterine Growth

    III. Nuclear Receptor Binding and RNA Polymerase Activity

    IV. Nuclear Retention and the Agonistic-Antagonistic Properties of Estriol

    V. Nuclear Retention and Replenishment of Estrogen Receptor and Hormone Antagonism

    VI. Long-Term Nuclear Retention and Acceptor Sites

    VII. Conclusion


    2 Conformational Forms of the Estrogen Receptor

    I. Introduction

    II. Transformation of the Rat Uterine Estrogen Receptor

    III. Kinetic Analysis of the Relationship of the 4 S to the 5 S Estrogen Receptor

    IV. Molecular Properties of the Estrogen Receptor from the Human Uterus

    V. Conformational Models of the Estrogen Receptor

    VI. Conclusion


    3 Nuclear Estrogen Receptor and DNA Synthesis

    I. Introduction

    II. Estrogen and the Cell Cycle

    III. Dynamics of DNA Synthesis in Response to Sequential Injections of Estrogen

    IV. Antimitotic Effects of Estrogen

    V. Conclusions


    4 The Role of Receptors in the Anabolic Action of Androgens

    I. Introduction

    II. Metabolism of Androgens by Mouse Kidney

    III. Androgen Receptors in Mouse Kidney

    IV. Androgen Receptors in Mice with Testicular Feminization (tfm)

    V. Effects of Androgen Receptors on RNA Polymerase and Chromatin Template Activation

    VI. Role of Androgen Receptors in the A jtion of Progestins on Mouse Kidney

    VII. Effects of Androgens on Kidney Growth

    VIII. Summary and Conclusions


    5 Androgen Receptors and Biologic Responses: A Survey

    I. Introduction

    II. General Model for the Mechanism of Action of Androgens

    III. Desirable Trends in Future Research

    IV. Summary


    6 Androgen Receptor Interactions in Target Cells: Biochemical Evaluation

    I. Evidence for Existence of Androgen Receptors

    II. Identification and Characterization of Androgen Receptors

    III. Specificities in Androgen-Receptor Interactions

    IV. Cell Nucleus and Chromatin Binding of Androgen Receptor

    V. Interaction of Androgen Receptors with Other Cellular Components

    VI. Concluding Remarks


    7 Biology of Progesterone Receptors

    I. Introduction

    II. Progesterone Action in the Hamster

    III. Progesterone Uptake In Vivo

    IV. Methods for Cytosol Progesterone Receptor

    V. Progesterone Receptor Distribution in Different Tissues

    VI. Regulation of Progesterone Receptor Levels

    VII. Progesterone Receptor Synthesis In Vitro


    8 Molecular Structure and Analysis of Progesterone Receptors

    I. Introduction

    II. The Progesterone Receptor Protein

    III. Effects of Progesterone in Vivo on Chromatin Gene Transcription

    IV. Effects of Purified Progesterone-Receptor Complexes In Vitro on Chromatin Gene Transcription

    V. A Proposed Model for Steroid Hormone Regulation of Gene Transcription


    9 Studies on the Cytoplasmic Glucocorticoid Receptor and Its Nuclear Interaction in Mediating Induction of Tryptophan Oxygenase Messenger RNA in Liver and Hepatoma

    I. Introduction

    II. Glucocorticoid Receptor

    III. Metabolic Effects of Glucocorticoids

    IV. Control of Specific Species of mRNA by Glucocorticoids

    V. Glucocorticoidal Control of the mRNA for Tryptophan Oxygenase in Hepatomas

    VI. Interaction of the Receptor with Nuclear Components

    VII. Conclusions


    10 Regulation of Gene Expression by Glucocorticoid Hormones: Studies of Receptors and Responses in Cultured Cells

    I. Introduction

    II. Glucocorticoid Hormone Receptors

    III. The Domain of Response to Glucocorticoid Hormones

    IV. Agonists, Partial Agonists, and Antagonists: Comparisons of Actions in Various Systems

    V. Structure-Activity Relations: Nature of the Receptor-Binding Site

    VI. Mechanism of Agonist and Antagonist Steroid Action: Allosteric Model for Steroid Hormone Action

    VII. Activation of the Receptor-Glucocorticoid Complex

    VIII. Return of the Receptor to the Cytosol: The First Step in Deinduction

    IX. Nuclear Binding of Receptor-Glucocorticoid Complexes

    X. Genetic Approaches to the Study of Glucocorticoid Hormone Action

    XI. Regulation of mRNA by Glucocorticoid Hormones

    XII. Deinduction of the Glucocorticoid Response: Posttranscriptional Control of Tyrosine Aminotransferase

    XIII. Mechanism of Glucocorticoid Receptor Action: Parallels with Cyclic AMP Action in Bacteria

    XIV. Summary


    11 Glucocorticoid Regulation of Mammary Tumor Virus Gene Expression

    I. Introduction: Defining the Problems

    II. Mammary Tumor Virus Genes in Murine Cells

    III. MTV RNA Induction Is a Receptor-Mediated Primary Hormone Response

    IV. Dexamethasone Stimulates the Rate of MTV RNA Synthesis

    V. Glucocorticoid-Responsive MTV Genes Are Mobile

    VI. MTV-Infected HTC Cells Contain Unintegrated Viral DNA

    VII. MTV Infection Alters Host Gene Response to Glucocorticoids

    VIII. Discussion


    12 Biology of Mineralocorticoid Receptors

    I. Introduction

    II. General Presence of [3H]Aldosterone in Target Cells

    III. Properties of the Cytosol Aldosterone Receptor

    IV. Properties of the Nuclear Aldosterone Receptor

    V. Evidence for a Receptor-Mediated Response


    13 Gonadal Steroid Receptors in Neuroendocrine Tissues

    I. Introduction

    II. Estradiol

    III. Testosterone

    IV. Progesterone

    V. Steroid Receptors and Sexual Differentiation of the Brain

    VI. Conclusion


    14 Hormones and Their Receptors in Breast Cancer

    I. Introduction

    II. Prolactin

    III. Estrogen

    IV. Progesterone

    V. Glucocorticoids

    VI. Androgens

    VII. Summary and Conclusions


    15 Steroid-Binding Serum Globulins: Recent Results

    I. Introduction

    II. Progesterone-Binding Globulin of the Pregnant Guinea Pig

    III. Kinetics of Steroid-Protein Interactions

    IV. On the Chemical Nature of the Binding Site


    16 Progesterone-Binding Proteins in Plasma and the Reproductive Tract

    I. Progesterone-Binding Plasma Proteins

    II. Progesterone Receptors

    III. Female Genital Tract Secretory Proteins

    IV. Discussion


    17 Androgen-Binding Proteins of the Male Rat Reproductive Tract

    I. Introduction

    II. Androgen-Binding Protein (ABP)

    III. 9 S Androgen- and Progesterone-Binding Protein

    IV. Androgen Receptor

    V. Concluding Remarks


    18 Vitamin 0 Receptors and Biologic Responses

    I. Introduction

    II. Receptors for Vitamin D

    III. Receptors for 25-(OH)D

    IV. Receptors for 1,25-(OH)2Da

    V. Summary


    19 Cellular-Binding Protein for Compounds with Vitamin A Activity

    I. Introduction

    II. The Vitamin A-Deficient Animal

    III. Vitamin A Acid (Retinoic Acid)

    IV. Fate of Vitamin A-Active Compounds in Vivo

    V. Vitamin A and Cellular Differentiation

    VI. Cellular Retinol-Binding Protein (CRBP)

    VII. Cellular Retinoic Acid-Binding Protein (CRABP)

    VIII. Properties of the Cellular-Binding Proteins

    IX. Other Vitamin A-Binding Proteins

    X. Cellular-Binding Proteins and Cancer

    XI. Conclusions



Product details

  • No. of pages: 618
  • Language: English
  • Copyright: © Academic Press 1978
  • Published: January 1, 1978
  • Imprint: Academic Press
  • eBook ISBN: 9781483262710

About the Editors

Bert W. O'Malley

Dr. Bert O’Malley was first to discover that nuclear receptors are transcription factors that regulate specific mRNA production in target cells in response to intracellular hormones. He uncovered mechanisms for activating steroid receptors, and discovered the existence of ‘coactivators’, the ‘master genes of transcription that regulate normal and disease functions in reproduction, growth and metabolism. He developed the concept that small molecule drugs can regulate coactivators to produce therapeutic outcomes for diseases such as cancer and heart disease. Dr. O’Malley is the founding father of the field of Molecular Endocrinology and a member of the National Academy of Sciences, National Academy of Medicine, and National Academy of Inventors.

Affiliations and Expertise

Thompson Distinguished Leadership Professor of MCB, Chancellor, Baylor College of Medicine, Houston, TX, USA

Lutz Birnbaumer

Affiliations and Expertise

School of Medicine, University of California, Los Angeles, U.S.A.

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