Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.

Détails

ID Serval
serval:BIB_CCAEC57D9943
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 of receptors coupled to guanine nucleotide regulatory proteins.
Périodique
Trends in Pharmacological Sciences
Auteur(s)
Lefkowitz R.J., Cotecchia S., Samama P., Costa T.
ISSN
0165-6147 (Print)
ISSN-L
0165-6147
Statut éditorial
Publié
Date de publication
1993
Volume
14
Numéro
8
Pages
303-307
Langue
anglais
Résumé
Adrenoceptors are prototypic members of the superfamily of seven transmembrane domain, G protein-coupled receptors. Study of the properties of several mutationally activated adrenoceptors is deepening understanding of the normal functioning of this ubiquitous class of receptors. The new findings suggest an expansion of the classical ternary complex model of receptor action to include an explicit isomerization of the receptors from an inactive to an active state which couples to the G protein ('allosteric ternary complex model'). This isomerization involves conformational changes which may occur spontaneously, or be induced by agonists or appropriate mutations which abrogate the normal 'constraining' function of the receptor, allowing it to 'relax' into the active conformation. Robert Lefkowitz and colleagues discuss the physiological and pathophysiological implications of these new insights into regulation of receptor activity.
Mots-clé
Amino Acid Sequence, Animals, GTP-Binding Proteins/metabolism, Models, Chemical, Molecular Sequence Data, Mutation, Receptors, Cell Surface/chemistry, Receptors, Cell Surface/metabolism, Stereoisomerism, Structure-Activity Relationship
Pubmed
Web of science
Création de la notice
24/01/2008 11:05
Dernière modification de la notice
20/08/2019 15:47
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