Constitutive activity in receptors and other Proteins, Part B [electronic resource].
- Author:
- Simon, Melvin I.
- Published:
- Academic Press [Imprint], Nov. 2010 San Diego : Elsevier Science & Technology Books.
- Physical Description:
- 708 pages : illustrations ; 09.000 x 06.000 in.
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- Contents:
- Machine generated contents note: Section I Inverse Agonism and Inverse Agonists -- 1.Identification and Characterization of Steroidogenic Factor-1 Inverse Agonists / Enzo Lalli -- 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 Sterold Production -- 4.Conclusion -- Acknowledgments -- References -- 2.Assessment of Inverse Agonism for the Angiotensin II Type 1 Receptor / Issei Komuro -- 1.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 -- 3.Measurement of Inverse Agonism in β-Adrenoceptors / Christian Hocht -- 1.Introduction: Basal Spontaneous Receptor Activity. The Rise of the Concept of Inverse Agonism -- 2.β-Adrenoceptors: Main Features -- 3.Methodological Aspects of the Assessment of Inverse Agonist Properties at βAR -- 4.Clinical Potential Uses of βAR Inverse Agonists -- References -- 4.Techniques for Studying Inverse Agonist Activity of Antidepressants at Recombinant Nonedited 5-HT2C-INI Receptor and Native Neuronal 5-HT2C Receptors / Philippe Marin -- 1.Introduction -- 2.Constitutive Activity Toward the Gαq-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 -- 5.Differential Inverse Agonism at the Human Muscarinic M3 Receptor / Remko A. Bakker -- 1.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 -- 6.Ghrelin Receptor: High Constitutive Activity and Methods for Developing Inverse Agonists / Constance Chollet -- 1.Introduction -- 2.Constitutive Activity and Development of Ghrelin Receptor Inverse Agonists -- 3.Synthesis of Ghrelin Receptor Inverse Agonists: Solid-Phase Peptide Synthesis (SPPS) -- 4.Functional Assays for Ghrelin Receptor Inverse Agonists -- References -- 7.Constitutive Activity and Inverse Agonism at the α1a and α1b Adrenergic Receptor Subtypes / Susanna Cotecchia -- 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 α1-ARs -- 5.Conclusions -- Acknowledgments -- References -- 8.Measurement of Inverse Agonism of the Cannabinoid Receptors / Tung M. Fong -- 1.Introduction -- 2.Gi-cAMP Assay -- 3.GTPγS Binding Assay -- 4.Electrophysiological Assays -- 5.Summary -- References -- 9.Constitutively Active Thyrotropin and Thyrotropin-Releasing Hormone Receptors and Their Inverse Agonists / Marvin C. Gershengorn -- 1.Introduction -- 2.TRH-R2 and Its Inverse Agonist Midazolam -- 3.TSHR and Its Inverse Agonist NCGC00161856 -- Acknowledgments -- References -- 10.Inverse Agonists and Antagonists of Retinoid Receptors / Hinrich Gronemeyer -- 1.Introduction -- 2.Functional Classification of Retinoid Receptor Ligands -- 3.Structural Basis of Retinoid Receptor Action -- 4.Synthetic Routes and Toolbox for Rational Retinoid Design -- 5.Protocols for the Study of Ligand Function -- 6.Chemical Syntheses -- Acknowledgments -- References -- 11.γ-Aminobutyric Acid Type A (GABAA) Receptor Subtype Inverse Agonists as Therapeutic Agents in Cognition / Ciciani Giovanna -- 1.Introduction -- 2.Inverse Agonism: Definition -- 3.Negative Allosteric Regulators of GABAA-R in Cognitive Impairment -- 4.Methods for Evaluating the Affinity and Efficacy at GABAA Receptor Subtypes -- 5.Conclusion -- References -- 12.Assays for Inverse Agonists in the Visual System / Masahiro Kono -- 1.Introduction -- 2.Opsin Preparation -- 3.Transducin Preparation -- 4.Transducin Activation Assay -- Acknowledgments -- References -- 13.Receptor-Driven Identification of Novel Human A3 Adenosine Receptor Antagonists as Potential Therapeutic Agents / Stefano Moro -- 1.Introduction -- 2.Newer Potential Therapeutic Role of A3 Adenosine Receptors -- 3.A3 Adenosine Receptor Antagonists -- 4.Receptor-Based Antagonist Design -- Acknowledgments -- References -- 14.Inverse Agonist Activity of Steroidogenic Factor SF-1 / Andria L. Del Tredici -- 1.Introduction -- 2.SF-1 Inverse Agonism in the R-SAT® Assay of Cellular Proliferation -- 3.SF-1 Inverse Agonism in Luciferase Transcriptional Assay -- 4.SF-1 Inverse Agonism in Adrenocortical Cultures -- Acknowledgments -- References -- 15.Methods to Measure G-Protein-Coupled Receptor Activity for the Identification of Inverse Agonists / Rafael Rodriguez-Puertas -- 1.Introduction -- 2.[35S]GTPγS Binding Assay in Membrane Homogenates -- 3.[35S]GTPγS Autoradiography in Brain Sections -- Acknowledgments -- References -- Section II Novel Strategies and Techniques for Constitutive Activity and Inverse Agonism -- 16.Use of Pharmacoperones to Reveal GPCR Structural Changes Associated with Constitutive Activation and Trafficking / P. Michael Conn -- 1.Introduction -- 2.Methods for Measuring Receptors and Receptor Activity -- 3.Assessment of Results -- 4.Conclusions -- Acknowledgments -- References -- 17.Application of Large-Scale Transient Transfection to Cell-Based Functional Assays for Ion Channels and GPCRs / Regina M. Reilly -- 1.Introduction -- 2.Large-Scale Transient Transfection -- 3.Cryopreservation of Cells -- 4.Application to Ion Channel Assays -- 5.Application to GPCR Assays -- 6.Conclusion -- Acknowledgment -- References -- 18.Quantification of RNA Editing of the Serotonin 2C Receptor (5-HT2CR) Ex Vivo / Kathryn A. Cunningham -- 1.RNA Editing of the 5-HT2CR -- 2.Functional Properties of 5-HT2CR Edited Isoforms -- 3.Current Methods for Quantification of 5-HT2CR Editing Events Ex Vivo -- 4.Quantification of 5-HT2CR Editing Events Ex Vivo with qRT-PCR -- Acknowledgments -- References -- 19.Strategies for Isolating Constitutively Active and Dominant-Negative Pheromone Receptor Mutants in Yeast / James B. Konopka -- 1.Introduction -- 2.Selecting a Yeast Strain and Expression Vector -- 3.Transforming Plasmids into Yeast -- 4."Gap-Repair" Approach for Targeting Mutagenesis to Genes on Plasmids -- 5.Isolation of Constitutively Active Mutants -- 6.Isolation of Dominant-Negative Mutants -- 7.Further Methods for Analysis of Mutant Receptors -- Acknowledgments -- References -- 20.Development of a GPR23 Cell-Based β-Lactamase Reporter Assay / Bonnie J. Hanson -- 1.Introduction -- 2.GPCR Cell-Based Assays -- 3.Development of a Cell-Based β-Lactamase Reporter Assay for Constitutively Active GPR23 -- 4.Identification of GPR23 Inverse Agonists Using a β-Lactamase Reporter Screen -- 5.Concluding Remarks -- Acknowledgments -- References -- 21.Computational Modeling of Constitutively Active Mutants of GPCRs: C5a Receptor / Thomas J. Baranski -- 1.Introduction -- 2.Modeling CAMs Based on Experimental Data for the Ground and Activated States of GPCRs -- 3.Rotational Sampling of the TM Regions of GPCRs -- 4.Modeling Structural Mechanisms of Constitutive Activity in C5aRs -- 5.Conclusions and Perspectives -- Acknowledgments -- References -- 22.TSH Receptor Monoclonal Antibodies with Agonist, Antagonist, and Inverse Agonist Activities / Bernard Rees Smith -- 1.Introduction -- 2.Production of Monoclonal Antibodies to the TSHR with the Characteristics of Patient Serum Autoantibodies -- 3.Characterization of 5C9 a Human Autoantibody with TSH Antagonist and TSHR Inverse Agonist Activity -- 4.Effects of TSHR Mutations on the Activity of MAb 5C9 -- 5.Structure of MAb 5C9 Fab -- 6.Conclusions -- Acknowledgment -- References -- 23.Current Standards, Variations, and Pitfalls for the Determination of Constitutive TSHR Activity In Vitro / Ralf Paschke -- 1.Introduction -- 2.Detection of Constitutive TSHR Activity -- 3.Methods and Required Materials for LRA -- 4.Conclusion -- Acknowledgment -- References -- 24.Toward the Rational Design of Constitutively Active KCa3.1 Mutant Channels / Remy Sauve -- 1.Introduction -- 2.Production of Constitutively Active KCa3.1 Mutant Channels -- 3.Concluding Remarks -- References -- 25.Fusion Proteins as Model Systems for the Analysis of Constitutive GPCR Activity / Roland Seifert -- 1.Introduction -- 2.Expression of Fusion Proteins: hH4R-Gα12 and hH4R-GAIP as Paradigms -- 3.Investigation of GPCR Constitutive Activity with Fusion Proteins: H4R as Paradigm -- 4.Application of the Fusion Protein Approach to other GPCRs -- Acknowledgments -- References -- 26.Screening for Novel Constitutively Active CXCR2 Mutants and Their Cellular Effects / Tim E. Sparer -- 1.Introduction -- 2.Establishment of a Yeast System to Identify CXCR2 CAMs -- 3.Establishment of a Mammalian System to Characterize CXCR2 CAMs -- References -- 27.A Method for Parallel Solid-Phase Synthesis of Iodinated Analogs of the Cannabinoid Receptor Type I (CB1) Inverse Agonist Rimonabant / Chih-Chung Tseng -- 1.Introduction -- 2.Concepts for Molecular Imaging -- 3.Conventional Methods for Preparation of Radiolabeled Pharmaceuticals for Imaging the CB1 Receptor -- 4.Parallel Solid-Phase Synthesis of lodinated Analogs of the CB1 Receptor Inverse Agonist Rimonabant -- 5.Materials and Methods -- References -- 28.Coexpression Systems as Models for the Analysis of Constitutive GPCR Activity / Roland Seifert -- 1.Introduction -- 2.Coexpression of GPCRs and Signaling Proteins: hH4R as Paradigm -- 3.Investigation of GPCR Constitutive Activity with Coexpression Systems -- and Contents note continued: 4.Application to Other Receptors -- Acknowledgments -- References -- 29.Modeling and Simulation of Inverse Agonism Dynamics / L.J. Bridge -- 1.Introduction -- 2.Single-Ligand Analysis -- 3.Two Competing Ligands -- 4.Discussion -- Acknowledgments -- References -- 30.Design and Use of Constitutively Active STAT5 Constructs / Michael A. Farrar -- 1.Introduction -- 2.Design of Constitutively Active STAT5 Constructs -- 3.Use of Constitutively Active STAT5 Constructs -- 4.Concerns with the Use of Constitutively Active STAT5 Constructs -- Acknowledgments -- References -- 31.In Vitro and In Vivo Assays of Protein Kinase CK2 Activity / Claude Cochet -- 1.Introduction -- 2.Monitoring of CK2 Catalytic Activity in Living Cells -- 3.Assays of CK2 Subunit Interaction -- 4.Visualization of CK2α-CK2β Interaction in Living Cells -- Acknowledgments -- References.
- Summary:
- Annotation
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
- Genre(s):
- ISBN:
- 9780123812964
0123812968 (Trade Cloth) - Audience Notes:
- Scholarly & Professional Elsevier Science & Technology Books
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