Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.

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