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Regulation of G Protein Coupled Receptor Function and Expression: Receptor Biochemistry and Methodology

Regulation of G Protein Coupled Receptor Function and Expression: Receptor Biochemistry and Methodology

Jeffrey L. Benovic

ISBN: 978-0-471-25277-1

Nov 1999

301 pages

Select type: Hardcover

In Stock



Recent advances in molecular and cell biology enabling the cloning, expression, and mutagenesis of signal transduction proteins has prompted an explosion of knowledge in the field of receptor regulation, facilitating the discovery of new classes of regulatory proteins, and providing a basis and means for manipulating receptor function through multiple intracellular targets.

This volume covers methods used to examine how the function(s) of receptors are regulated. Understanding how to regulate the function and expression of these receptors is critical in determining how to modify receptors and to translocating receptors away from the cell surface and its recycling.

Individual chapters focus on specific techniques used to characterize receptors (epitope tagging, measurement and analysis of receptor phosphorylation, analysis of the kinetics of receptor desensitization, and assessment of receptor/G protein coupling); the role of regulatory proteins (receptor kinases and phosphatases, arrestins) in modulating receptor function; and the methods used to measure receptor trafficking (ligand binding, immunofluoresence) and expression (transcriptional and translational regulation).
* Covers a broad range of important concepts and methodologies which are current in the study of G protein-coupled receptors (GPCRs)
* G-protein coupled receptors make up over 40% of the current pharmacological targets
* Provides detailed protocols for executing various strategies and offers informed judgments as to what approaches are and aren't useful
* Volume Editor, Jeffrey Benovic, is a dominant world leader in the study of receptor regulation of GPCR kinases and is highly respected in the field

Epitope Tagging and Detection Methods for Receptor Identification (U. Klein & M. von Zastrow).

Measurement of Receptor Phosphorylation in Situ (M. Bouvier, et al.).

Reconstitution and in vitro Phosphorylation of G Protein-Coupled Receptors (J. Ptasienski & M. Hosey).

Identification of Residues that are Phosphorylated within a Receptor (K. Palczewski, et al.).

Palmitoylation of G Protein-Coupled Receptors (H. Jin, et al.).

Assays for Measuring Receptor/G Protein Coupling (Q. Li & R. Cerione).


Expression and Activity of G Protein-Coupled Receptor Kinases (R. Loudon, et al.).

Characterization of Arrestin Expression and Function (V. Gurevich, et al.).

The G Protein-Coupled Receptor Phosphatase (J. Pitcher & R. Lefkowitz).


Radioligand Binding Assays for G Protein-Coupled Receptor Internalization (M. Toews).

Characterization of Receptor Sequestration by Immunofluorescent Microscopy (F. Santini & J. Keen).

Characterization of Receptor Trafficking Using Green Fluorescent Protein (N. Tarasova, et al.).

The Analysis of Post-Transciptional Regulation of the Expression of G Protein-Coupled Receptors (B. Tholanikunnel & C. Malbon).