Receptors and Hormone Action

Receptors and Hormone Action

Volume III

1st Edition - January 1, 1978

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  • Editors: Lutz Birnbaumer, Bert W. O'Malley
  • eBook ISBN: 9781483262727

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Receptors and Hormone Action, Volume III, 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. This book opens with a chapter on the physiological properties of the thyroid hormone receptors in the intact animal. This is followed by separate chapters on β-adrenergic receptors; the study of hormone-receptor interaction by measuring the biological responses induced by the actions of gonadotropins on Leydig cells; chemical and immunochemical properties of hCG and PMSG treated with glycosidases; and binding of follitropin (FSH) to rat testes. Subsequent chapters deal with the control of changes of gonadotropin responsiveness of the granulosa cell during follicular maturation; regulation of prolactin receptors by steroid hormones; and the role of membrane protein phosphorylation in the effects of neurotransmitters.

Table of Contents

  • List of Contributors


    Contents of Previous Volumes

    1 Nuclear Receptors for Triiodothyronine: A Physiological Perspective

    I. Introduction: Thyroid Hormone Deficiency and Excess

    II. Dynamics of T3 Bound to Nuclear Sites

    III. Physiological Role of the Nuclear T3 Binding Site

    IV. The Possibility of Other Initiating Sites

    V. Speculations on Molecular Mechanisms

    VI. Concluding Remarks


    2 In Vitro Studies on Thyroid Hormone Receptors

    I. Introduction

    II. Cell Culture Considerations

    III. Effect of Thyroid Hormones in Cultured GHX Cells

    IV. Quantitation of Growth Hormone mRNA and Regulation of Glucocorticoid Action by Thyroid Hormone in GH1 Cells

    V. Are There Extranuclear Actions of Thyroid Hormone?

    VI. Summary and Conclusions


    3 Regulation of Gene Expression by Thyroid Hormones

    I. Introduction

    II. Thyroid Hormone "Receptors"

    III. Studies on the Nuclear Localization of the Receptors

    IV. Hormonal Control of Receptor Levels?

    V. Characteristics of the Solubilized Receptors

    VI. Chromatin Fractionation Studies

    VII. The Receptor as a DNA-Binding Protein

    VIII. A Macromolecular Factor Is Required for the Specificity of Hormone Recognition by the Recepto

    IX. Biological Activities of Various Thyroid Hormones: The Role of Cellular MetabolisM

    X. Thyroid Hormones Regulate Specific Messenger RNA Levels

    XI. Model for Thyroid Hormone Action


    4 Direct Identification and Characterization of ß-Adrenergic Receptors and Functional Relationship of Adenylyl Cyclase

    I. Introduction

    II. Chemistry of HYP and I-HYP

    III. [125I]HYP Binding to ß-Adrenergic Receptors

    IV. Direct Analysis of Interaction of Agonists and Antagonists with ß-Adrenergic Receptors Employing [125I]HYP

    V. Determination of Kt and Ka for Inhibition or Activation of Adenylyl Cyclase

    VI. Effects of Guanine Nucleotides

    VII. Structure-Function Relationships

    VIII. Relationship between Receptor Binding, Adenylyl Cyclase Activity, and Biological Effects

    IX. Nature of the Functional Relationship of ß-Andrenergic Receptors and Adenylyl Cyclase

    X. Summary


    5 Heart ß-Andrenoceptors

    I. Introduction

    II. Theory

    III. Tissue Uptake of Catecholamines

    IV. Affinity of Ligands for Cardiac ß-Adrenoceptors

    V. Apparent Dissociation of Adenylyl Cyclase Stimulation from Other Myocardial Effects of Adrenergic Ligands

    VI. Comments


    6 Regulation of ß-Adrenergic Receptors by ß-Adrenergic Agonists

    I. Introduction

    II. Methods for Direct Study of ß-Adrenergic Receptors

    III. Catecholamine Desensitization in the Frog Erythrocyte Model System-In Vivo Studies

    IV. In Vitro Desensitization Studies

    V. Studies in a Cell-Free System

    VI. A Model of Catecholamine Desensitization in the Frog Erythrocyte


    7 Regulation of ß-Adrenergic Function in the Rat Pineal Gland

    I. ß-Adrenergic Stimulation of Melatonin Synthesis

    II. Regulation of Sensitivity to ß-Adrenergic Stimulation

    III. Conclusion


    8 A Model for Peptide Hormone Action Based upon Measurement of Functional Hormone Binding

    I. Introduction

    II. The Functional Binding Procedure

    III. Computer Stimulations of H-N Plots for Selected Models of Binding-Response Coupling

    IV. Experimental Results

    V. Kinetics of Functional Binding: Threshold

    VI. Cooperativity in Binding and Response

    VII. Summary and Conclusions

    VIII. Statistical Appendix


    9 Role of Carbohydrate in the Action of Gonadotropins

    I. Introduction

    II. Carbohydrate Structures of Gonadotropins Revealed by Sequential Degradation with Glycosidases

    III. Immunologic Properties of Glycosidase-Treated Derivatives of hCG and PMSG

    IV. Mechanism of Gonadotropin Action after Carbohydrate Removal

    V. Models of Hormone Action and Role of Cyclic AMP as a Mediator of Steroidogenesis


    10 Gonadotropin Receptors and Regulation of Interstitial Cell Function in the Testis

    I. Introduction

    II. Gonadotropin Receptors

    III. Gonadotropin Binding and Regulation of Leydig Cell Responses

    IV. Hormonal Regulation of Gonadotropin Receptors


    11 Follitropin Receptors in Rat Testis Tubule Membranes: Characterization, Solubilization, and Study of Factors Affecting Interaction with FSH

    I. Introduction

    II. Preparation of Purified Rat Tubule Membranes

    III. Binding of [125I]hFSH to Subcellular Fractions of Rat Tubules

    IV. Binding of [125I]hFSH to Rat Tubule Plasma Membranes

    V. Effects of Nucleotides on the Binding and Dissociation of [125I]hFSH

    VI. Properties of the Follitropin Receptor in Purified Tubule Membranes

    VII. Inhibition of FSH Binding to Tubule Membrane Receptor

    VIII. Solubilization of Follitropin Receptors in Rat Testes


    12 Mechanism of Action of FSH in the Male Rat

    I. Introduction

    II. Membrane Receptors for FSH

    III. Effects on Cyclic Nucleotide Metabolism

    IV. Stimulation of Translation and Transcription

    V. Modulation of Androgen Binding Protein Activity

    VI. Concluding Remarks


    13 Physiological Aspects of Appearance and Desensitization of Gonadotropin-Sensitive Adenylyl Cyclase in Ovarian Tissues and Membranes of Rabbits, Rats, and Pigs

    I. Introduction

    II. Desensitization of Adenylyl Cyclase to LH Stimulation in Graafian Follicles

    III. Desensitization of Adenylyl Cyclase to LH Stimulation in Corpora Lutea

    IV. Desensitization of Adenylyl Cyclase to LH Stimulation in Membrane Particles

    V. Concluding Remarks

    VI. Appendix


    14 Development and Hormonal Regulation of Gonadotropin Responsiveness in Granulosa Cells of the Mammalian Ovary

    I. Introduction

    II. Changes in Granulosa Cells during Follicular Maturation

    III. Induction of the Luteinized State in Vitro in Granulosa Cells Obtained from Immature Small Follicles

    IV. Role of Steroid Hormones in Granulosa Cell Luteinization

    V. Granulosa Cell Atresia

    VI. Intraovarian Inhibitors

    VII. Summary


    15 Regulation of Prolactin Receptors by Steroid Hormones and Use of Radioligand Assays in Endocrine Research

    I. Introduction: Binding Studies and Radioreceptor Assays

    II. Hepatic Receptors for Lactogenic Hormones

    III. Prolactin Receptor Induction in the Testes and Prostate Gland

    IV. Prolactin Receptor in the Ovaries—A Synergism of Luteotropin Receptor Induction

    V. Prolactin Receptor Induction in the Mammary Gland

    VI. Prolactin Receptors in the Adrenal Gland and Kidney

    VII. Prolactin Receptors in Mammary Carcinomas

    VIII. Conclusion


    16 Hormone Regulation of Ovarian Hormone Receptors



    17 Interactions of TRH, LH-RH, and Somatostatin in the Anterior Pituitary Gland

    I. Introduction

    II. Role of Cyclic AMP in the Action of Hypothalamic Hormones

    III. [3H]TRH Binding in Anterior Pituitary Tissue

    IV. Modulation of Pituitary TRH Receptors

    V. Interactions between TRH and Somatostatin for TSH and PRL Release

    VI. Modulation of LH and FSH Responses to LH-RH by Androgens and Estrogens

    VII. LH-RH Analogues


    18 Brain Receptors for Neurotransmitters

    I. Introduction

    II. The Problem

    III. Acetylcholine

    IV. Dopamine

    V. GABA

    VI. Glutamate and Aspartate

    VII. Glycine

    VIII. Norepinephrine

    IX. Opiates

    X. Serotonin

    XI. Conclusion


    19 The Mechanism of Opiate Agonist and Antagonist Action

    I. Introduction

    II. Biochemical Basis of the Sodium Effect

    III. Endogenous Ligands for the Opiate Receptor

    IV. The Opiate Receptor In Vivo


    20 Hormonal Regulation of Cyclic Nucleotide Phosphodiesterases

    I. Introduction

    II. General Considerations

    III. Techniques and Applications

    IV. Insulin Activation of Cyclic Nucleotide Phosphodiesterase


    21 Phosphorylation of Membrane Proteins in the Actions of Hormones and Neurotransmitters

    I. Introduction

    II. Evidence for a Role of Membrane Protein Phosphorylation in the Effects of Neurotransmitters

    III. Evidence Suggesting a Role for Membrane Phosphorylation in Hormonal Control of Permeability and Transport

    IV. Membrane Protein Phosphorylation Serving Other Functions

    V. Conclusions and Speculation on Future Research



Product details

  • No. of pages: 648
  • Language: English
  • Copyright: © Academic Press 1978
  • Published: January 1, 1978
  • Imprint: Academic Press
  • eBook ISBN: 9781483262727

About the Editors

Lutz Birnbaumer

Affiliations and Expertise

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

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

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