Constitutively active mutants of the beta1-adrenergic receptor.

Détails

ID Serval
serval:BIB_A7244D8C5E1D
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Titre
Constitutively active mutants of the beta1-adrenergic receptor.
Périodique
FEBS Letters
Auteur(s)
Lattion A., Abuin L., Nenniger-Tosato M., Cotecchia S.
ISSN
0014-5793 (Print)
ISSN-L
0014-5793
Statut éditorial
Publié
Date de publication
1999
Volume
457
Numéro
3
Pages
302-306
Langue
anglais
Résumé
We provide the first evidence that point mutations can constitutively activate the beta(1)-adrenergic receptor (AR). Leucine 322 of the beta(1)-AR in the C-terminal portion of its third intracellular loop was replaced with seven amino acids (I, T, E, F, C, A and K) differing in their physico-chemical properties. The beta(1)-AR mutants expressed in HEK-293 cells displayed various levels of constitutive activity which could be partially inhibited by some beta-blockers. The results of this study might have interesting implications for future studies aiming at elucidating the activation process of the beta(1)-AR as well as the mechanism of action of beta-blockers.
Mots-clé
Adrenergic beta-1 Receptor Agonists, Adrenergic beta-2 Receptor Agonists, Adrenergic beta-Agonists/metabolism, Adrenergic beta-Agonists/pharmacology, Adrenergic beta-Antagonists/metabolism, Adrenergic beta-Antagonists/pharmacology, Amino Acid Substitution, Betaxolol/metabolism, Betaxolol/pharmacology, Carbazoles/metabolism, Carbazoles/pharmacology, Cell Line/drug effects, Cell Line/metabolism, Cyclic AMP/metabolism, Epinephrine/metabolism, Epinephrine/pharmacology, Humans, Imidazoles/metabolism, Imidazoles/pharmacology, Isoproterenol/metabolism, Isoproterenol/pharmacology, Labetalol/metabolism, Labetalol/pharmacology, Point Mutation, Practolol/metabolism, Practolol/pharmacology, Propanolamines/metabolism, Propanolamines/pharmacology, Receptors, Adrenergic, beta-1/genetics, Receptors, Adrenergic, beta-1/metabolism, Receptors, Adrenergic, beta-2/metabolism, Recombinant Proteins/genetics, Recombinant Proteins/metabolism, Timolol/metabolism, Timolol/pharmacology
Pubmed
Web of science
Open Access
Oui
Création de la notice
24/01/2008 11:05
Dernière modification de la notice
20/08/2019 15:12
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