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G-Protein-Coupled Receptors in Heart Disease.

Publication ,  Journal Article
Wang, J; Gareri, C; Rockman, HA
Published in: Circ Res
August 31, 2018

GPCRs (G-protein [guanine nucleotide-binding protein]-coupled receptors) play a central physiological role in the regulation of cardiac function in both health and disease and thus represent one of the largest class of surface receptors targeted by drugs. Several antagonists of GPCRs, such as βARs (β-adrenergic receptors) and Ang II (angiotensin II) receptors, are now considered standard of therapy for a wide range of cardiovascular disease, such as hypertension, coronary artery disease, and heart failure. Although the mechanism of action for GPCRs was thought to be largely worked out in the 80s and 90s, recent discoveries have brought to the fore new and previously unappreciated mechanisms for GPCR activation and subsequent downstream signaling. In this review, we focus on GPCRs most relevant to the cardiovascular system and discuss traditional components of GPCR signaling and highlight evolving concepts in the field, such as ligand bias, β-arrestin-mediated signaling, and conformational heterogeneity.

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Published In

Circ Res

DOI

EISSN

1524-4571

Publication Date

August 31, 2018

Volume

123

Issue

6

Start / End Page

716 / 735

Location

United States

Related Subject Headings

  • Ventricular Remodeling
  • Ventricular Function
  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Myocytes, Smooth Muscle
  • Myocytes, Cardiac
  • Humans
  • Heart Ventricles
  • Heart Failure
  • Fibroblasts
 

Citation

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Wang, J., Gareri, C., & Rockman, H. A. (2018). G-Protein-Coupled Receptors in Heart Disease. Circ Res, 123(6), 716–735. https://doi.org/10.1161/CIRCRESAHA.118.311403
Wang, Jialu, Clarice Gareri, and Howard A. Rockman. “G-Protein-Coupled Receptors in Heart Disease.Circ Res 123, no. 6 (August 31, 2018): 716–35. https://doi.org/10.1161/CIRCRESAHA.118.311403.
Wang J, Gareri C, Rockman HA. G-Protein-Coupled Receptors in Heart Disease. Circ Res. 2018 Aug 31;123(6):716–35.
Wang, Jialu, et al. “G-Protein-Coupled Receptors in Heart Disease.Circ Res, vol. 123, no. 6, Aug. 2018, pp. 716–35. Pubmed, doi:10.1161/CIRCRESAHA.118.311403.
Wang J, Gareri C, Rockman HA. G-Protein-Coupled Receptors in Heart Disease. Circ Res. 2018 Aug 31;123(6):716–735.

Published In

Circ Res

DOI

EISSN

1524-4571

Publication Date

August 31, 2018

Volume

123

Issue

6

Start / End Page

716 / 735

Location

United States

Related Subject Headings

  • Ventricular Remodeling
  • Ventricular Function
  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Myocytes, Smooth Muscle
  • Myocytes, Cardiac
  • Humans
  • Heart Ventricles
  • Heart Failure
  • Fibroblasts