Historical review: Negative efficacy and the constitutive activity of G-protein-coupled receptors.

Détails

ID Serval
serval:BIB_35CE1A293E46
Type
Article: article d'un périodique ou d'un magazine.
Sous-type
Synthèse (review): revue aussi complète que possible des connaissances sur un sujet, rédigée à partir de l'analyse exhaustive des travaux publiés.
Collection
Publications
Titre
Historical review: Negative efficacy and the constitutive activity of G-protein-coupled receptors.
Périodique
Trends in Pharmacological Sciences
Auteur(s)
Costa T., Cotecchia S.
ISSN
0165-6147 (Print)
ISSN-L
0165-6147
Statut éditorial
Publié
Date de publication
2005
Volume
26
Numéro
12
Pages
618-624
Langue
anglais
Résumé
The idea that a receptor can produce signalling without agonist intervention and that several antagonists can be 'active' in repressing such spontaneous activity is contained in the concept of ligand-induced conformational changes. Yet, this idea was neglected by pharmacologists for many years. In this article, we review the events that brought inverse agonism and constitutive activity to general attention and made this phenomenon a topic of current research. We also suggest a classification of antagonists based on the cooperativity that links their primary site of interaction with other functional domains of the receptor.
Mots-clé
Animals, Humans, Ligands, Receptors, G-Protein-Coupled/agonists, Receptors, G-Protein-Coupled/antagonists & inhibitors, Signal Transduction
Pubmed
Web of science
Création de la notice
24/01/2008 11:05
Dernière modification de la notice
20/08/2019 13:23
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