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Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.

Publication ,  Journal Article
Lefkowitz, RJ; Cotecchia, S; Samama, P; Costa, T
Published in: Trends Pharmacol Sci
August 1993

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.

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Published In

Trends Pharmacol Sci

DOI

ISSN

0165-6147

Publication Date

August 1993

Volume

14

Issue

8

Start / End Page

303 / 307

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Stereoisomerism
  • Receptors, Cell Surface
  • Pharmacology & Pharmacy
  • Mutation
  • Molecular Sequence Data
  • Models, Chemical
  • GTP-Binding Proteins
  • Animals
  • Amino Acid Sequence
 

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Lefkowitz, R. J., Cotecchia, S., Samama, P., & Costa, T. (1993). Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci, 14(8), 303–307. https://doi.org/10.1016/0165-6147(93)90048-O
Lefkowitz, R. J., S. Cotecchia, P. Samama, and T. Costa. “Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.Trends Pharmacol Sci 14, no. 8 (August 1993): 303–7. https://doi.org/10.1016/0165-6147(93)90048-O.
Lefkowitz RJ, Cotecchia S, Samama P, Costa T. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci. 1993 Aug;14(8):303–7.
Lefkowitz, R. J., et al. “Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins.Trends Pharmacol Sci, vol. 14, no. 8, Aug. 1993, pp. 303–07. Pubmed, doi:10.1016/0165-6147(93)90048-O.
Lefkowitz RJ, Cotecchia S, Samama P, Costa T. Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins. Trends Pharmacol Sci. 1993 Aug;14(8):303–307.
Journal cover image

Published In

Trends Pharmacol Sci

DOI

ISSN

0165-6147

Publication Date

August 1993

Volume

14

Issue

8

Start / End Page

303 / 307

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Stereoisomerism
  • Receptors, Cell Surface
  • Pharmacology & Pharmacy
  • Mutation
  • Molecular Sequence Data
  • Models, Chemical
  • GTP-Binding Proteins
  • Animals
  • Amino Acid Sequence