Constitutive activity and inverse agonism at the α(₁a) and α(₁b) adrenergic receptor subtypes.

Détails

ID Serval
serval:BIB_20924BE99A14
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Titre
Constitutive activity and inverse agonism at the α(₁a) and α(₁b) adrenergic receptor subtypes.
Périodique
Methods in Enzymology
Auteur(s)
Cotecchia S.
ISSN
1557-7988 (Electronic)
ISSN-L
0076-6879
Statut éditorial
Publié
Date de publication
2010
Volume
485
Pages
123-138
Langue
anglais
Résumé
The α(1b)-adrenergic receptor (AR) was, after rhodopsin, the first G protein-coupled receptor (GPCR) in which point mutations were shown to trigger constitutive (agonist-independent) activity. Constitutively activating mutations have been found in other AR subtypes as well as in several GPCRs. This chapter briefly summarizes the main findings on constitutively active mutants of the α(1a)- and α(1b)-AR subtypes and the methods used to predict activating mutations, to measure constitutive activity of Gq-coupled receptors and to investigate inverse agonism. In addition, it highlights the implications of studies on constitutively active AR mutants on elucidating the molecular mechanisms of receptor activation and drug action.
Mots-clé
Animals, Drug Inverse Agonism, Humans, Mutagenesis, Site-Directed/methods, Mutation, Protein Structure, Tertiary, Receptors, Adrenergic, alpha-1/chemistry, Receptors, Adrenergic, alpha-1/genetics
Pubmed
Web of science
Création de la notice
11/03/2011 17:55
Dernière modification de la notice
20/08/2019 12:56
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