UID:
almafu_9958130980102883
Umfang:
1 online resource (721 p.)
Ausgabe:
1st ed.
ISBN:
9786612954856
,
9781282954854
,
1282954857
,
9780123812971
,
0123812976
Serie:
Methods in enzymology ; v. 485
Inhalt:
This volume of Methods in Enzymology covers the current methodology for the detection and assessment of constitutively active proteins. The chapters written by expert authors who are leaders in the field, provide hints and tricks not available in primary research publications.It is extensively referenced, with useful figures and tables throughout the volume. A. Expert authors who are leaders in the field B. Extensively referenced and useful figures and tables C. Provides hints and tricks to facilitate reproduction of methods
Anmerkung:
Description based upon print version of record.
,
Front Cover; Methods in Enzymology: Constitutive Activity in Receptors and Other Proteins, Part B; Copyright Page; Contents; Contributors; Preface; Volume in Series; Section One: Inverse Agonism and Inverse Agonists; Chapter 1: Identification and Characterization of Steroidogenic Factor-1 Inverse Agonists; 1. Introduction; 2. Characterization of Inverse Agonists of SF-1 by uHTS; 3. Effect of SF-1 Inverse Agonists on Adrenocortical Tumor Cell Proliferation and Steroid Production; 4. Conclusion; Acknowledgments; References
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Chapter 2: Assessment of Inverse Agonism for the Angiotensin II Type 1 Receptor1. Introduction; 2. Protocol for Cell Culture and Transfection; 3. Radioligand Assay for AT1 Receptor; 4. Protocol for Cell Stretching; 5. Assessment of AT1 Receptor Activation; 6. Conclusion; Acknowledgments; References; Chapter 3: Measurement of Inverse Agonism in beta-Adrenoceptors; 1. Introduction: Basal Spontaneous Receptor Activity. The Rise of the Concept of Inverse Agonism; 2. beta-Adrenoceptors: Main Features; 3. Methodological Aspects of the Assessment of Inverse Agonist Properties at betaAR
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4. Clinical Potential Uses of betaAR Inverse AgonistsReferences; Chapter 4: Techniques for Studying Inverse Agonist Activity of Antidepressants at Recombinant Nonedited 5-HT2C-INI Receptor and Native Neuronal 5-HT2CReceptors; 1. Introduction; 2. Constitutive Activity Toward the Gaq-PLC Effector Pathway of 5-HT2C-INI Receptors Transiently Expressed in HEK-293 Cells; 3. Plasma Membrane Insertion of 5-HT2C-INI Receptors; 4. Enhanced Responsiveness of Constitutively Active 5-HT2C Receptors Upon Prolonged Treatment with Inverse Agonists; Acknowledgments; References
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Chapter 5: Differential Inverse Agonism at the Human Muscarinic M3 Receptor1. Introduction to Muscarinic Receptors; 2. Role of M3R in Regulating Smooth Muscle Function and Clinical Use of Anticholinergics; 3. In Vitro Assays to Monitor hM3R Activation and Constitutive Activity; 4. Constitutive Activity and Receptor Upregulation Studies; 5. Physiological Relevance of hM3R Constitutive Activity; References; Chapter 6: Ghrelin Receptor: High Constitutive Activity and Methods for Developing Inverse Agonists; 1. Introduction
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2. Constitutive Activity and Development of Ghrelin Receptor Inverse Agonists3. Synthesis of Ghrelin Receptor Inverse Agonists: Solid-Phase Peptide Synthesis (SPPS); 4. Functional Assays for Ghrelin Receptor Inverse Agonists; References; Chapter 7: Constitutive Activity and Inverse Agonism at the a1a and a1b Adrenergic Receptor Subtypes; 1. Introduction; 2. Combination of Computational Modeling and Site-Directed Mutagenesis of the Receptor to Identify Constitutively Activating Mutations; 3. Measuring Constitutive Activity of Receptor-Mediated Gq Activation; 4. Inverse Agonism at the a1-ARs
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5. Conclusions
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English
Weitere Ausg.:
ISBN 9780123812964
Weitere Ausg.:
ISBN 0123812968
Sprache:
Englisch
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