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Receptors and Hormone Action - 1st Edition - ISBN: 9780125263030, 9781483262727

Receptors and Hormone Action

1st Edition

Volume III

Editors: Lutz Birnbaumer Bert O'Malley
eBook ISBN: 9781483262727
Imprint: Academic Press
Published Date: 1st January 1978
Page Count: 648
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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


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




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

About the Editors

Lutz Birnbaumer

Affiliations and Expertise

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

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

Ratings and Reviews