Chapter 6. The Impact of G Proteins on Constitutive GPCR Activity

  1. Prof. Roland Seifert2 and
  2. Prof. Thomas Wieland3
  1. Graeme Milligan

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch6

G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24

G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24

How to Cite

Milligan, G. (2005) The Impact of G Proteins on Constitutive GPCR Activity, in G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity, Volume 24 (eds R. Seifert and T. Wieland), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/352760734X.ch6

Editor Information

  1. 2

    Department of Pharmacology and Toxicology, University of Regensburg, Universitätsstraße 31, D-93053 Regensburg, Germany

  2. 3

    Institut für Pharmakologie und Toxikologie, Fakultät für Klinische Medizin Mannheim der Universität Heidelberg, Maybachstraße 14-16, 68169 Mannheim, Germany

Author Information

  1. Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, United Kingdom

Publication History

  1. Published Online: 25 APR 2006
  2. Published Print: 26 SEP 2005

Book Series:

  1. Methods and Principles in Medicinal Chemistry

Book Series Editors:

  1. Prof. Dr. Raimund Mannhold4,
  2. Prof. Dr. Hugo Kubinyi5 and
  3. Prof. Dr. Gerd Folkers6

Series Editor Information

  1. 4

    Biomedical Research Center, Molecular Drug Research Group, Heinrich-Heine-Universität, Universitätsstrasse 1, 40225 Düsseldorf, Germany

  2. 5

    Donnersbergstrasse 9, 67256 Weisenheim am Sand, Germany

  3. 6

    Collegium Helveticum, STW/ETH Zentrum, 8092 Zürich, Switzerland

ISBN Information

Print ISBN: 9783527308194

Online ISBN: 9783527607341

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Keywords:

  • G protein coupled receptors (GPCR);
  • contribution of G proteins to constitutive activity;
  • GPCR–G protein fusion proteins

Summary

This chapter contains sections titled:

  • Introduction

  • The Contribution of G proteins to Constitutive Activity

    • Basic Features

    • The Distribution of G Proteins in the Plasma Membrane

  • GPCR–G Protein Fusion Proteins

    • Basic Features

    • Modulation of the GPCR–G Protein Interface Alters Constitutive Activity

    • Use of G Protein Variation to Detect Ligand Efficacy

  • Conclusions