Constitutive activity in receptors and other proteins, Part A / edited by P. Michael Conn.

Format:

Book

Contributor:

Conn, P. Michael.

Series:

Methods in enzymology ; v. 484.

Methods in enzymology ; v. 484

Language:

English

Subjects (All):

Proteins.

Cell receptors.

Physical Description:

1 online resource (821 p.)

Edition:

1st ed.

Place of Publication:

Amsterdam, Netherlands ; Boston, Mass. : Elsevier/Academic, 2010.

Language Note:

English

Summary:

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

Contents:

Front Cover; Methods Inenzymology: Constitutive Activity inReceptors and OtherProteins, Part A; Copyright; Contents; Contributors; Preface; Methods in Enzymology; Section One: Identification and Measurement of Constitutive Activity; Chapter 1: Constitutive Activity at the Cannabinoid CB1 Receptor and Behavioral Responses; 1. Introduction; 2. Modifying CB1 Activity; 3. Behavioral Models; References; Chapter 2: Detecting Constitutive Activity and Protean Agonism at Cannabinoid-2 Receptor; 1. Introduction; 2. General Considerations; 3. Evaluation of Constitutive Activity Using GTPgammaS Assay

4. Evaluation of Constitutive Activity Using cAMP Assay5. Evaluation of Constitutive Activity Using RT-CES; 6. Evaluation of Protean Agonism with cAMP Assay; 7. Comparison of the Methods; References; Chapter 3: Modulation of the Constitutive Activity of the Ghrelin Receptor by Use of Pharmacological Tools and Mutagenesis...; 1. Introduction; 2. The Ghrelin Receptor and Its Constitutive Activity; 3. Structural Basis of Constitutive Activity; 4. Residues Responsible for the Inverse Agonism and Efficacy Swap; 5. Physiological Relevance of Constitutive Activity; 6. Experimental Procedures

ReferencesChapter 4: Assessment of Constitutive Activity and Internalization of GPR54 (KISS1-R); 1. Introduction; 2. Materials; 3. Methods; Acknowledgments; References; Chapter 5: Assessment of Constitutive Activity in E-Type Prostanoid Receptors; 1. Introduction; 2. Assays Used to Assess EP3 Receptor Constitutive Activity; 3. Assays Used to Assess EP4 Receptor Constitutive Activity; References; Chapter 6: α1D-Adrenergic Receptors: Constitutive Activity and Reduced Expression at the Plasma Membrane; 1. Introduction; 2. Methods; 3. Constitutive Activity

4. Plasma Membrane α1D-Adrenergic Receptors5. Possible Physiological Implications; Acknowledgments; References; Chapter 7: Constitutive Activity of the Histamine H1 Receptor; 1. Introduction; 2. Methods to Study Constitutive H1R Signaling; 3. Constitutive Activity as Tool to Elucidate Receptor Activation and Crosstalk; 4. Conclusion; Acknowledgments; References; Chapter 8: Constitutive Activity of Somatostatin Receptor Subtypes; 1. Introduction; 2. Choosing Cells to be Studied; 3. Modifying SSTR Density; 4. Summary; References

Chapter 9: Assessment of Homologous Internalization of Constitutively Active N111G Mutant of AT1 Receptor1. Introduction; 2. Preparation of Receptor Plasmid and Protein; 3. Radioligand Binding Assay; 4. Inositol Phosphate Accumulation Assay; 5. Internalization Assay; 6. Western Blot Analysis; 7. Data Analysis; 8. Concluding Remark; References; Chapter 10: Methods to Detect Cell Surface Expression and Constitutive Activity of GPR6; 1. Introduction; 2. GPR6 is Expressed in Intracellular Compartments; 3. Comparison of the Cell Surface Protein Detection Methods

4. Comparison of the Constitutive Gs-Activity Detection Methods

Notes:

Description based upon print version of record.

Includes bibliographical references and indexes.

ISBN:

9786612954863

9781282954861

1282954865

9780123812995

0123812992

OCLC:

701703976