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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

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

Published Date

  • September 3, 1996

Published In

Volume / Issue

  • 93 / 18

Start / End Page

  • 9954 - 9959

PubMed ID

  • 8790438

Pubmed Central ID

  • PMC38536

International Standard Serial Number (ISSN)

  • 0027-8424

Digital Object Identifier (DOI)

  • 10.1073/pnas.93.18.9954


  • eng

Conference Location

  • United States