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Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning.

Publication ,  Journal Article
Frielle, T; Caron, MG; Lefkowitz, RJ
Published in: Clin Chem
May 1989

The beta 1- and beta 2-adrenergic receptor subtypes are biochemically and functionally similar, because both receptors mediate the catecholamine-dependent activation of adenylate cyclase through the GTP-binding protein, Gs. Pharmacologically, the two receptors can be distinguished on the basis of their relative affinities for the agonists epinephrine and norepinephrine as well as their affinities for several selective antagonists. The primary structures of the human beta 1- and beta 2-adrenergic receptors have recently been deduced from the cloning of their genes and (or) cDNAs, revealing high sequence homology and a membrane topography of seven putative transmembrane regions similar to that of rhodopsin. Chimeric beta 1/beta 2-adrenergic receptor cDNAs have been constructed by site-directed mutagenesis and the chimeric RNA transcripts expressed in Xenopus laevis oocytes. The pharmacological properties of the expressed chimeric receptor proteins were assessed by radioligand binding utilizing subtype-selective agonists and antagonists. Apparently, several of the putative transmembrane regions contribute significantly to the determination of subtype selectivity, presumably by formation of a ligand-binding pocket, with determinants for agonist and antagonist binding being distinguishable.

Duke Scholars

Published In

Clin Chem

ISSN

0009-9147

Publication Date

May 1989

Volume

35

Issue

5

Start / End Page

721 / 725

Location

England

Related Subject Headings

  • Xenopus
  • Recombinant Proteins
  • Receptors, Adrenergic, beta
  • General Clinical Medicine
  • Cloning, Molecular
  • Binding Sites
  • Animals
  • 3205 Medical biochemistry and metabolomics
  • 3202 Clinical sciences
  • 1103 Clinical Sciences
 

Citation

APA
Chicago
ICMJE
MLA
NLM
Frielle, T., Caron, M. G., & Lefkowitz, R. J. (1989). Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. Clin Chem, 35(5), 721–725.
Frielle, T., M. G. Caron, and R. J. Lefkowitz. “Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning.Clin Chem 35, no. 5 (May 1989): 721–25.
Frielle T, Caron MG, Lefkowitz RJ. Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. Clin Chem. 1989 May;35(5):721–5.
Frielle, T., et al. “Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning.Clin Chem, vol. 35, no. 5, May 1989, pp. 721–25.
Frielle T, Caron MG, Lefkowitz RJ. Properties of the beta 1- and beta 2-adrenergic receptor subtypes revealed by molecular cloning. Clin Chem. 1989 May;35(5):721–725.

Published In

Clin Chem

ISSN

0009-9147

Publication Date

May 1989

Volume

35

Issue

5

Start / End Page

721 / 725

Location

England

Related Subject Headings

  • Xenopus
  • Recombinant Proteins
  • Receptors, Adrenergic, beta
  • General Clinical Medicine
  • Cloning, Molecular
  • Binding Sites
  • Animals
  • 3205 Medical biochemistry and metabolomics
  • 3202 Clinical sciences
  • 1103 Clinical Sciences