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Myocardial G protein-coupled receptor kinases: implications for heart failure therapy.

Publication ,  Journal Article
Iaccarino, G; Lefkowitz, RJ; Koch, WJ
Published in: Proc Assoc Am Physicians
1999

The beta-adrenergic signaling cascade is an important regulator of myocardial function. Significant alterations of this pathway are associated with several cardiovascular diseases, including congestive heart failure (CHF). Included in these alterations is increased activity and expression of G protein-coupled receptor kinases (GRKs), such as the beta-adrenergic receptor kinase (beta ARK1), which phosphorylate and desensitize beta-adrenergic receptors (beta ARs). A body of evidence is accumulating that suggests that GRKs, in particular beta ARK1, are critical determinants of cardiac function under normal conditions and in disease states. Transgenic mice with myocardial-targeted alterations of GRK activity have shown profound changes in the in vivo functional performance of the heart. Included in these studies is the compelling finding that inhibition of beta ARK1 activity or expression significantly enhances cardiac function and potentiates beta AR signaling in failing cardiomyocytes. This article summarizes the advances made in the study of beta ARK1 in the heart and addresses its potential as a novel therapeutic target for CHF.

Duke Scholars

Published In

Proc Assoc Am Physicians

DOI

ISSN

1081-650X

Publication Date

1999

Volume

111

Issue

5

Start / End Page

399 / 405

Location

United States

Related Subject Headings

  • beta-Adrenergic Receptor Kinases
  • Sympathetic Nervous System
  • Signal Transduction
  • Receptors, Adrenergic, beta
  • Protein Serine-Threonine Kinases
  • Myocardium
  • Mice, Transgenic
  • Mice
  • Humans
  • Heart Failure
 

Citation

APA
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ICMJE
MLA
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Iaccarino, G., Lefkowitz, R. J., & Koch, W. J. (1999). Myocardial G protein-coupled receptor kinases: implications for heart failure therapy. Proc Assoc Am Physicians, 111(5), 399–405. https://doi.org/10.1111/paa.1999.111.5.399
Iaccarino, G., R. J. Lefkowitz, and W. J. Koch. “Myocardial G protein-coupled receptor kinases: implications for heart failure therapy.Proc Assoc Am Physicians 111, no. 5 (1999): 399–405. https://doi.org/10.1111/paa.1999.111.5.399.
Iaccarino G, Lefkowitz RJ, Koch WJ. Myocardial G protein-coupled receptor kinases: implications for heart failure therapy. Proc Assoc Am Physicians. 1999;111(5):399–405.
Iaccarino, G., et al. “Myocardial G protein-coupled receptor kinases: implications for heart failure therapy.Proc Assoc Am Physicians, vol. 111, no. 5, 1999, pp. 399–405. Pubmed, doi:10.1111/paa.1999.111.5.399.
Iaccarino G, Lefkowitz RJ, Koch WJ. Myocardial G protein-coupled receptor kinases: implications for heart failure therapy. Proc Assoc Am Physicians. 1999;111(5):399–405.

Published In

Proc Assoc Am Physicians

DOI

ISSN

1081-650X

Publication Date

1999

Volume

111

Issue

5

Start / End Page

399 / 405

Location

United States

Related Subject Headings

  • beta-Adrenergic Receptor Kinases
  • Sympathetic Nervous System
  • Signal Transduction
  • Receptors, Adrenergic, beta
  • Protein Serine-Threonine Kinases
  • Myocardium
  • Mice, Transgenic
  • Mice
  • Humans
  • Heart Failure