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Direct demonstration of impaired functionality of a purified desensitized beta-adrenergic receptor in a reconstituted system.

Publication ,  Journal Article
Strulovici, B; Cerione, RA; Kilpatrick, BF; Caron, MG; Lefkowitz, RJ
Published in: Science
August 24, 1984

Long-term exposure of various cell types to beta-adrenergic agonists such as isoproterenol leads to an attenuated responsiveness ("desensitization") of the adenylate cyclase system to further challenge with these agonists. The turkey erythrocyte model system was used earlier to show that a covalent modification of the receptor (phosphorylation) is associated with this process. The functionality of the "desensitized" beta-adrenergic receptor was assessed by implanting purified beta-adrenergic receptor preparations from control and desensitized turkey erythrocytes into phospholipid mixtures and then fusing them with receptor-deficient cells (Xenopus laevis erythrocytes). Desensitized beta-adrenergic receptors showed a 40 to 50 percent reduction in their ability to couple to the heterologous adenylate cyclase system, comparable to the reduction in their functionality observed in their original membrane environment. These results demonstrate the utility of recently developed receptor reconstitution techniques for assessing the functionality of purified receptors and show a direct link between a covalent modification of a membrane-bound receptor and its impaired functionality in a reconstituted system.

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Published In

Science

DOI

ISSN

0036-8075

Publication Date

August 24, 1984

Volume

225

Issue

4664

Start / End Page

837 / 840

Location

United States

Related Subject Headings

  • Xenopus laevis
  • Turkeys
  • Receptors, Adrenergic, beta
  • Phosphorylation
  • Norepinephrine
  • Membrane Fusion
  • Liposomes
  • Isoproterenol
  • General Science & Technology
  • Erythrocytes
 

Citation

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Strulovici, B., Cerione, R. A., Kilpatrick, B. F., Caron, M. G., & Lefkowitz, R. J. (1984). Direct demonstration of impaired functionality of a purified desensitized beta-adrenergic receptor in a reconstituted system. Science, 225(4664), 837–840. https://doi.org/10.1126/science.6089331
Strulovici, B., R. A. Cerione, B. F. Kilpatrick, M. G. Caron, and R. J. Lefkowitz. “Direct demonstration of impaired functionality of a purified desensitized beta-adrenergic receptor in a reconstituted system.Science 225, no. 4664 (August 24, 1984): 837–40. https://doi.org/10.1126/science.6089331.
Strulovici B, Cerione RA, Kilpatrick BF, Caron MG, Lefkowitz RJ. Direct demonstration of impaired functionality of a purified desensitized beta-adrenergic receptor in a reconstituted system. Science. 1984 Aug 24;225(4664):837–40.
Strulovici, B., et al. “Direct demonstration of impaired functionality of a purified desensitized beta-adrenergic receptor in a reconstituted system.Science, vol. 225, no. 4664, Aug. 1984, pp. 837–40. Pubmed, doi:10.1126/science.6089331.
Strulovici B, Cerione RA, Kilpatrick BF, Caron MG, Lefkowitz RJ. Direct demonstration of impaired functionality of a purified desensitized beta-adrenergic receptor in a reconstituted system. Science. 1984 Aug 24;225(4664):837–840.
Journal cover image

Published In

Science

DOI

ISSN

0036-8075

Publication Date

August 24, 1984

Volume

225

Issue

4664

Start / End Page

837 / 840

Location

United States

Related Subject Headings

  • Xenopus laevis
  • Turkeys
  • Receptors, Adrenergic, beta
  • Phosphorylation
  • Norepinephrine
  • Membrane Fusion
  • Liposomes
  • Isoproterenol
  • General Science & Technology
  • Erythrocytes