Regulation of G Protein Coupled Receptor Function and Expression

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 fieldDieser umfassende Band beschreibt viele der aktuell angewandten Techniken zur Bestimmung der molekularen Mechanismen, die bei der Rezeptorregulation eine Rolle spielen. Behandelt wird ein breites Spektrum wichtiger Grundlagen und Methoden für die Analyse von G Protein-gekoppelten Rezeptoren. Geschrieben von anerkannten Experten auf diesem Gebiet. (01/00) 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.

Jeffrey L. Benovic is the author of Regulation of G Protein Coupled Receptor Function and Expression: Receptor Biochemistry and Methodology, published by Wiley. G protein-coupled receptors (GPCRs) constitute the largest single class of receptors and are responsible for mediating much of intracellular mammalian signaling. Indeed, over 40 percent of the pharmacological targets being evaluated by drug companies are related to G protein-coupled receptors. Understanding how GPCRs are regulated is critical in determining waysto control their function and expression. This volume covers basic concepts while providing comprehensive treatment of methods used to examine how the functions of GPCRs are regulated.

Chapters in this volume, edited by Dr. Jeffrey Benovic, a world-renowned expert in the study of GPCR regulation, describe:
* Current techniques used to define the molecular mechanisms involved in receptor regulation
* ;Specific techniques employed to characterize receptors
* The role of regulatory proteins in modulating receptor function
* Methods used to measure receptor trafficking and expression

Covering a broad range of fundamental concepts and methodologies which are current in the study of GPCRs, Regulation of G Protein-Coupled Receptor Function and Expression is a vital reference for receptor biochemists, pharmacologists, neuroscientists, molecular biologists, cell biologists, and physiologists.

Also in this series:

Receptor Localization: Laboratory Methods and Procedures edited by Marjorie A. Ariano

Identification and Expression of G Protein-Coupled Receptors
edited by Kevin R. Lynch

Structure-Function Analysis of G Protein-Coupled Receptors
edited by Jürgen Wess