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

Details

Serval ID
serval:BIB_20924BE99A14
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Constitutive activity and inverse agonism at the α(₁a) and α(₁b) adrenergic receptor subtypes.
Journal
Methods in Enzymology
Author(s)
Cotecchia S.
ISSN
1557-7988 (Electronic)
ISSN-L
0076-6879
Publication state
Published
Issued date
2010
Volume
485
Pages
123-138
Language
english
Abstract
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.
Keywords
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
Create date
11/03/2011 17:55
Last modification date
20/10/2020 14:41
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