Scholars@Duke publication: Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice.

Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice.

Publication , Journal Article

Rockman, HA; Choi, DJ; Rahman, NU; Akhter, SA; Lefkowitz, RJ; Koch, WJ

Published in: Proc Natl Acad Sci U S A

September 3, 1996

Published version (DOI) Open Access Copy (Duke) Link to item

Transgenic mice were generated with cardiac-specific overexpression of the G protein-coupled receptor kinase-5 (GRK5), a serine/threonine kinase most abundantly expressed in the heart compared with other tissues. Animals overexpressing GRK5 showed marked beta-adrenergic receptor desensitization in both the anesthetized and conscious state compared with nontransgenic control mice, while the contractile response to angiotensin II receptor stimulation was unchanged. In contrast, the angiotensin II-induced rise in contractility was significantly attenuated in transgenic mice overexpressing the beta-adrenergic receptor kinase-1, another member of the GRK family. These data suggest that myocardial overexpression of GRK5 results in selective uncoupling of G protein-coupled receptors and demonstrate that receptor specificity of the GRKs may be important in determining the physiological phenotype.

Duke Scholars

Author Robert J. Lefkowitz Medicine, Cardiology

Author Howard Allan Rockman Medicine, Cardiology

Altmetric Attention Stats

Dimensions Citation Stats

Published In

Proc Natl Acad Sci U S A

DOI

10.1073/pnas.93.18.9954

ISSN

0027-8424

Publication Date

September 3, 1996

Volume

Issue

Start / End Page

9954 / 9959

Location

United States

Related Subject Headings

beta-Adrenergic Receptor Kinases
Receptors, Angiotensin
Receptors, Adrenergic, beta
Receptor Protein-Tyrosine Kinases
RNA, Messenger
Protein Serine-Threonine Kinases
Phenotype
Myocardium
Myocardial Contraction
Mice, Transgenic

Citation

APA

Chicago

ICMJE

MLA

NLM

Rockman, H. A., Choi, D. J., Rahman, N. U., Akhter, S. A., Lefkowitz, R. J., & Koch, W. J. (1996). Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice. Proc Natl Acad Sci U S A, 93(18), 9954–9959. https://doi.org/10.1073/pnas.93.18.9954

Rockman, H. A., D. J. Choi, N. U. Rahman, S. A. Akhter, R. J. Lefkowitz, and W. J. Koch. “Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice.” Proc Natl Acad Sci U S A 93, no. 18 (September 3, 1996): 9954–59. https://doi.org/10.1073/pnas.93.18.9954.

Rockman HA, Choi DJ, Rahman NU, Akhter SA, Lefkowitz RJ, Koch WJ. Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice. Proc Natl Acad Sci U S A. 1996 Sep 3;93(18):9954–9.

Rockman, H. A., et al. “Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice.” Proc Natl Acad Sci U S A, vol. 93, no. 18, Sept. 1996, pp. 9954–59. Pubmed, doi:10.1073/pnas.93.18.9954.

Published In

Proc Natl Acad Sci U S A

DOI

10.1073/pnas.93.18.9954

ISSN

0027-8424

Publication Date

September 3, 1996

Volume

Issue

Start / End Page

9954 / 9959

Location

United States

Related Subject Headings

beta-Adrenergic Receptor Kinases
Receptors, Angiotensin
Receptors, Adrenergic, beta
Receptor Protein-Tyrosine Kinases
RNA, Messenger
Protein Serine-Threonine Kinases
Phenotype
Myocardium
Myocardial Contraction
Mice, Transgenic