Constitutive activity and inverse agonism at the alpha1adrenoceptors.

Détails

ID Serval
serval:BIB_A3A81F7D34BE
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
Constitutive activity and inverse agonism at the alpha1adrenoceptors.
Périodique
Biochemical Pharmacology
Auteur(s)
Cotecchia S.
ISSN
0006-2952 (Print)
ISSN-L
0006-2952
Statut éditorial
Publié
Date de publication
2007
Volume
73
Numéro
8
Pages
1076-1083
Langue
anglais
Résumé
Mutations of G protein-coupled receptors (GPCR) can increase their constitutive (agonist-independent) activity. Some of these mutations have been artificially introduced by site-directed mutagenesis, others occur spontaneously in human diseases. The alpha(1B)adrenoceptor was the first GPCR in which point mutations were shown to trigger receptor activation. This article briefly summarizes some of the findings reported in the last several years on constitutive activity of the alpha(1)adrenoceptor subtypes, the location where mutations have been found in the receptors, the spontaneous activity of native receptors in recombinant as well as physiological systems. In addition, it will highlight how the analysis of the pharmacological and molecular properties of the constitutively active adrenoceptor mutants provided an important contribution to our understanding of the molecular mechanisms underlying the mechanism of receptor activation and inverse agonism.
Mots-clé
Adrenergic alpha-1 Receptor Antagonists, Adrenergic alpha-Antagonists/pharmacology, Amino Acid Sequence, Animals, COS Cells, Cercopithecus aethiops, Cricetinae, GTP-Binding Proteins/metabolism, Humans, Models, Molecular, Molecular Sequence Data, Mutation, Protein Conformation, Protein Structure, Secondary, Receptors, Adrenergic, alpha-1/chemistry, Receptors, Adrenergic, alpha-1/genetics, Receptors, G-Protein-Coupled/metabolism
Pubmed
Web of science
Création de la notice
24/01/2008 12:05
Dernière modification de la notice
03/03/2018 20:12
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