Chapter 3. Molecular Mechanisms of GPCR Activation

  1. Prof. Roland Seifert2 and
  2. Prof. Thomas Wieland3
  1. Søren G. F. Rasmussen and
  2. Ulrik Gether

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch3

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

Rasmussen, S. G. F. and Gether, U. (2005) Molecular Mechanisms of GPCR Activation, 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.ch3

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 Neuropharmacology Group, Dept. of Pharmacology 16–18, Panum Inst., University of Copenhagen, 2200 Copenhagen N, Denmark

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

SEARCH

Keywords:

  • G protein coupled receptors (GPCR);
  • molecular mechanisms;
  • structure;
  • ligand recognition;
  • conformational changes;
  • active receptor state;
  • stabilizing intramolecular interactions;
  • kinetics of agonist binding;
  • kinetics of receptor activation

Summary

This chapter contains sections titled:

  • Introduction

  • GPCR Structure and Ligand Recognition

  • Conformational Changes in the GPCR Activation Process

  • Conversion to the Active Receptor State Involves Release of Stabilizing Intramolecular Interactions

  • Kinetics of Agonist Binding and Receptor Activation

  • GPCR Activation in an Oligomeric Context