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Receptors and Hormone Action - 1st Edition - ISBN: 9780125263023, 9781483262710

Receptors and Hormone Action

1st Edition

Volume II

Editors: Bert O'Malley Lutz Birnbaumer
eBook ISBN: 9781483262710
Imprint: Academic Press
Published Date: 1st January 1978
Page Count: 618
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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




No. of pages:
© Academic Press 1978
1st January 1978
Academic Press
eBook ISBN:

About the Editors

Bert 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.

Ratings and Reviews