Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs

Laurent Prézeau; Cyril Goudet; Philippe Rondard; Jean‐Philippe Pin

doi:10.1002/3527608249.ch4

Retour

Chapitre d'ouvrage

Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs

Laurent Prézeau, Cyril Goudet, Philippe Rondard et Jean‐Philippe Pin

Ligand Design for G Protein‐coupled Receptors, pp.61-82

Methods and Principles in Medicinal Chemistry, Wiley‐VCH Verlag GmbH & Co. KGaA

20/01/2006

DOI: https://doi.org/10.1002/3527608249.ch4

Résumé

agonists activate class C GPCRs by stabilizing the closed state of the VFT

asymmetric functioning of the HD dimer

class C GPCRs

class C GPCRs are constitutive dimers

class C GPCRs are multidomain proteins

dimeric functioning of the dimer of VFTs

heptahelical domain

importance of GPCR dimerization for function

This chapter contains sections titled: Introduction Class C GPCRs are Multidomain Proteins The VFT The CRD The HD C‐Tail Class C GPCRs are Constitutive Dimers Agonists Activate Class C GPCRs by Stabilizing the Closed State of the VFT Dimeric Functioning of the Dimer of VFTs Agonist Stoichiometry: Symmetry or Asymmetry? The Heptahelical Domain, the Target of Positive and Negative Allosteric Modulators, Behaves in a Manner Similar to Rhodopsin‐like Class A GPCRs Allosteric Coupling Between the Extracellular and Heptahelical Domains within the Dimer Molecular Determinants of the Coupling Between the VFT and the HD Cis‐ and Trans‐activation Can Exist within Class C GPCRs Asymmetric Functioning of the HD Dimer Conclusion

Indicateurs

1 Consultations de la notice

Détails

Titre: Importance of GPCR Dimerization for Function: The Case of the Class C GPCRs
Créateurs - sans rôle: Laurent Prézeau
Cyril Goudet
Philippe Rondard
Jean‐Philippe Pin
Contributeurs - sans rôle: Didier Rognan - Laboratoire de Pharmacochimie de la Communication Cellulaire, CNRS UMR 7175‐LC1, Institut Gilbert Laustriat, 74, route du Rhin, 67401 Illkirch, France
Détails de publication: Ligand Design for G Protein‐coupled Receptors, pp.61-82
Publications en série: Methods and Principles in Medicinal Chemistry
Éditeur: Wiley‐VCH Verlag GmbH & Co. KGaA; Weinheim, FRG
Nombre de pages: 22
Identifiants: 99139540909311
Unité académique: Institut de Génomique Fonctionnelle - IGF
Langue: English
Type de ressource: Book chapter