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Regulation of G Protein-Coupled Receptor Function and Expression / Edition 1

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Overview

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

G Protein-Coupled receptors (GCPRs) are the largest single class of receptors in biology. They are responsible for mediating the intercellular signalling of almost all small, and some large molecules in mammals. Over 40% of the current pharmacological targets being evaluated by drug companies are related to GCPRs. 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 and translocate receptors away from the cell surface and its recycling.

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Product Details

  • ISBN-13: 9780471252771
  • Publisher: Wiley
  • Publication date: 11/28/1999
  • Series: Receptor Biochemistry and Methodology Series , #4
  • Edition description: New Edition
  • Edition number: 1
  • Pages: 301
  • Product dimensions: 7.20 (w) x 10.00 (h) x 0.90 (d)

Table of Contents

TECHNIQUES FOR CHARACTERIZING RECEPTOR FUNCTION.

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).

PROTEINS THAT REGULATE RECEPTOR FUNCTION.

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).

REGULATION OF RECEPTOR TRAFFICKING AND EXPRESSION.

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).

Index.

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