G-Protein-Coupled Receptors in Heart Disease.

Journal Article (Journal Article;Review)

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.

Full Text

Duke Authors

Cited Authors

  • Wang, J; Gareri, C; Rockman, HA

Published Date

  • August 31, 2018

Published In

Volume / Issue

  • 123 / 6

Start / End Page

  • 716 - 735

PubMed ID

  • 30355236

Pubmed Central ID

  • PMC6205195

Electronic International Standard Serial Number (EISSN)

  • 1524-4571

Digital Object Identifier (DOI)

  • 10.1161/CIRCRESAHA.118.311403


  • eng

Conference Location

  • United States