Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.
Journal Article (Journal Article;Review)
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.
Full Text
Duke Authors
Cited Authors
- Lefkowitz, RJ; Cotecchia, S; Samama, P; Costa, T
Published Date
- August 1993
Published In
Volume / Issue
- 14 / 8
Start / End Page
- 303 - 307
PubMed ID
- 8249148
International Standard Serial Number (ISSN)
- 0165-6147
Digital Object Identifier (DOI)
- 10.1016/0165-6147(93)90048-O
Language
- eng
Conference Location
- England