Chapter 4. Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity

  1. Prof. Roland Seifert2 and
  2. Prof. Thomas Wieland3
  1. Joël Bockaert,
  2. Sylvie Claeysen,
  3. Lara Joubert,
  4. Laurent Fagni and
  5. Aline Dumuis

Published Online: 25 APR 2006

DOI: 10.1002/352760734X.ch4

G Protein‐Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity

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

How to Cite

Bockaert, J., Claeysen, S., Joubert, L., Fagni, L. and Dumuis, A. (2005) Molecular and Cellular Determinants of GPCR Splice Variant Constitutive Activity, in G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity (eds R. Seifert and T. Wieland), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/352760734X.ch4

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. CNRS UPR9023, CCIPE, 141 rue de la Cardonille, 34094 Montpellier Cedex 05, France

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 determinants;
  • cellular determinants;
  • GPCR splice variants;
  • constitutive activation;
  • second messenger production;
  • constitutive internalization;
  • C-t GPCR splice variants

Summary

This chapter contains sections titled:

  • Introduction

  • Constitutive Activation of Second Messenger Production by C-Terminal Splice Variants of GPCRs

    • The Constitutive Activities of C-Terminal 5-HT4 Receptor Splice Variants: the Shortest, the Strongest

    • The Constitutive Activities of mGlu1R and mGlu5R C-t Splice Variants: a Case for which a Physiological Control does exist

    • Other Examples of GPCR C-t Splice Variants with Different Constitutive Activities

  • Differential Constitutive Internalization of C-t GPCR Splice Variants

    • The Thromboxane A2 Receptor TPβR, but not the TPαR Splice Variant, is Constitutively Internalized by Clathrin-dependent, GRK- and Arrestin-independent Mechanisms

    • The Prostaglandin F Receptor FPBR, but not the FPAR C-Terminal Splice Variant, is Constitutively Internalized by a Clathrin-independent, PI3-Kinase-dependent Mechanism.

  • Conclusion