Related Experiment Video

Updated: Jul 26, 2025

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators

Published on: February 20, 2018

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Role of G-protein coupled receptors in cardiovascular diseases

Yuanqiang Li1, Boyu Li2, Wei-Dong Chen3,4

  • 1State Key Laboratory of Chemical Resource Engineering, College of Life Science and Technology, Beijing University of Chemical Technology, Beijing, China.

Frontiers in Cardiovascular Medicine
|June 21, 2023
PubMed

Insights

G-protein-coupled receptors (GPCRs) are crucial in cardiovascular diseases (CVDs), influencing heart and vascular functions. Understanding GPCRs offers new therapeutic targets for treating these widespread conditions.

Area of Science:

  • Pharmacology
  • Cardiology
  • Molecular Biology

Background:

  • Cardiovascular diseases (CVDs) are the leading global cause of mortality, responsible for approximately 30% of annual deaths worldwide.
  • G-protein-coupled receptors (GPCRs) are integral cell surface receptors critical for regulating physiological and pathological cellular processes.
  • Existing CVD treatments, including beta-blockers, and a significant portion of cardiovascular drugs target GPCRs, highlighting their therapeutic importance.

Purpose of the Study:

  • To review and discuss the multifaceted roles of GPCRs in cardiovascular system function, encompassing both vascular and cardiac perspectives.
  • To analyze the complex regulatory mechanisms of multiple GPCRs in the context of vascular and heart diseases.
  • To identify novel therapeutic strategies and drug development opportunities for CVDs based on GPCR research.

Main Methods:

  • Literature review and synthesis of existing research on GPCR structure and function in cardiovascular contexts.
  • Analysis of data linking GPCR activity to cardiovascular physiology and pathology.
  • Exploration of therapeutic interventions targeting GPCRs for CVD treatment.

Main Results:

  • GPCRs play a pivotal role in regulating cardiovascular system functions, affecting both the heart and vasculature.
  • Evidence indicates that numerous GPCRs are implicated in the development and progression of various cardiovascular diseases.
  • Targeting GPCRs has proven effective in current CVD therapies and represents a significant area for future drug development.

Conclusions:

  • GPCRs are indispensable regulators of cardiovascular health and disease.
  • A comprehensive understanding of GPCRs in cardiovascular diseases is essential for advancing treatment options.
  • This review provides a foundation for developing innovative drugs targeting GPCRs to combat cardiovascular diseases effectively.

Keywords:
G-protein-coupled receptorscardiovascular diseasesheart functionischemia-reperfusionvascular tone

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