Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.

Details

Serval ID
serval:BIB_CCAEC57D9943
Type
Article: article from journal or magazin.
Publication sub-type
Review (review): journal as complete as possible of one specific subject, written based on exhaustive analyses from published work.
Collection
Publications
Institution
Title
Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.
Journal
Trends in Pharmacological Sciences
Author(s)
Lefkowitz R.J., Cotecchia S., Samama P., Costa T.
ISSN
0165-6147 (Print)
ISSN-L
0165-6147
Publication state
Published
Issued date
1993
Volume
14
Number
8
Pages
303-307
Language
english
Abstract
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.
Keywords
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
Create date
24/01/2008 12:05
Last modification date
20/08/2019 16:47
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