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Substitution of an extracellular cysteine in the beta 2-adrenergic receptor enhances agonist-promoted phosphorylation and receptor desensitization.

Publication ,  Journal Article
Liggett, SB; Bouvier, M; O'Dowd, BF; Caron, MG; Lefkowitz, RJ; DeBlasi, A
Published in: Biochem Biophys Res Commun
November 30, 1989

We constructed and expressed in a permanent cell line a beta 2-adrenergic receptor with a valine substitution for cysteine 184 of the second putative extracellular loop. The mutant receptor was partially uncoupled from adenylyl cyclase with impaired ability to form the high affinity agonist-receptor-G protein complex, yet displayed more rapid and extensive agonist-induced desensitization. The enhanced desensitization was accompanied by increased agonist promoted, but not cAMP promoted, receptor phosphorylation in intact cells. Thus, not only is impaired desensitization associated with decreased phosphorylation, as we have shown with several mutant beta 2-adrenergic receptors recently, but enhanced desensitization is accompanied by increased agonist promoted receptor phosphorylation. In the case of this cysteine mutant, this may be due to the greater accessibility of the uncoupled receptor for phosphorylation by the beta-adrenergic receptor kinase.

Duke Scholars

Published In

Biochem Biophys Res Commun

DOI

ISSN

0006-291X

Publication Date

November 30, 1989

Volume

165

Issue

1

Start / End Page

257 / 263

Location

United States

Related Subject Headings

  • Valine
  • Transfection
  • Receptors, Adrenergic, beta
  • Phosphorylation
  • Mutation
  • Kinetics
  • Isoproterenol
  • DNA
  • Cysteine
  • Cloning, Molecular
 

Citation

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Liggett, S. B., Bouvier, M., O’Dowd, B. F., Caron, M. G., Lefkowitz, R. J., & DeBlasi, A. (1989). Substitution of an extracellular cysteine in the beta 2-adrenergic receptor enhances agonist-promoted phosphorylation and receptor desensitization. Biochem Biophys Res Commun, 165(1), 257–263. https://doi.org/10.1016/0006-291x(89)91063-2
Liggett, S. B., M. Bouvier, B. F. O’Dowd, M. G. Caron, R. J. Lefkowitz, and A. DeBlasi. “Substitution of an extracellular cysteine in the beta 2-adrenergic receptor enhances agonist-promoted phosphorylation and receptor desensitization.Biochem Biophys Res Commun 165, no. 1 (November 30, 1989): 257–63. https://doi.org/10.1016/0006-291x(89)91063-2.
Liggett SB, Bouvier M, O’Dowd BF, Caron MG, Lefkowitz RJ, DeBlasi A. Substitution of an extracellular cysteine in the beta 2-adrenergic receptor enhances agonist-promoted phosphorylation and receptor desensitization. Biochem Biophys Res Commun. 1989 Nov 30;165(1):257–63.
Liggett, S. B., et al. “Substitution of an extracellular cysteine in the beta 2-adrenergic receptor enhances agonist-promoted phosphorylation and receptor desensitization.Biochem Biophys Res Commun, vol. 165, no. 1, Nov. 1989, pp. 257–63. Pubmed, doi:10.1016/0006-291x(89)91063-2.
Liggett SB, Bouvier M, O’Dowd BF, Caron MG, Lefkowitz RJ, DeBlasi A. Substitution of an extracellular cysteine in the beta 2-adrenergic receptor enhances agonist-promoted phosphorylation and receptor desensitization. Biochem Biophys Res Commun. 1989 Nov 30;165(1):257–263.
Journal cover image

Published In

Biochem Biophys Res Commun

DOI

ISSN

0006-291X

Publication Date

November 30, 1989

Volume

165

Issue

1

Start / End Page

257 / 263

Location

United States

Related Subject Headings

  • Valine
  • Transfection
  • Receptors, Adrenergic, beta
  • Phosphorylation
  • Mutation
  • Kinetics
  • Isoproterenol
  • DNA
  • Cysteine
  • Cloning, Molecular