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A Rat Model of Pressure Overload Induced Moderate Remodeling and Systolic Dysfunction as Opposed to Overt Systolic Heart Failure
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Molecular signaling of G-protein-coupled receptor in chronic heart failure and associated complications

Mohammad Altamish1, Vijaya Paul Samuel2, Rajiv Dahiya3

  • 1Department of Pharmacology, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India.

Drug Development Research
|December 1, 2019
PubMed

Insights

Heart failure impairs the heart

Area of Science:

  • Cardiology
  • Molecular Biology
  • Biochemistry

Background:

  • Heart failure is a clinical syndrome where the myocardium's pumping ability is compromised.
  • Adrenoceptors, particularly beta subtypes (β1, β2, β3), regulate cardiac activity.
  • Dysregulation of the ACE1/Ang II/AT1 and ACE2/Ang (1-7)/Mas receptor axes is implicated in heart failure.

Purpose of the Study:

  • To investigate the molecular mechanisms by which G-protein-coupled receptor kinases (GRKs) affect cardiac function during heart failure.
  • To explore the role of GRK2 and GRK5 in receptor desensitization and internalization in failing hearts.

Main Methods:

  • Review and analysis of existing clinical and preclinical data.
  • Examination of molecular signaling pathways involving adrenoceptors and the renin-angiotensin system.
  • Focus on the role of G-protein-coupled receptor kinases (GRKs) in cardiac dysfunction.

Main Results:

  • Increased activity of G-protein-coupled receptor kinases (GRK2 and GRK5) leads to desensitization and internalization of key receptors.
  • This process disrupts normal G-protein-mediated signaling crucial for cardiac regulation.
  • Altered GRK levels significantly impact cardiac activity in the context of heart failure.

Conclusions:

  • G-protein-coupled receptor kinases (GRKs) play a critical role in the molecular pathophysiology of heart failure.
  • Targeting GRK activity may offer a novel therapeutic strategy for managing heart failure.
  • Understanding GRK-mediated signaling is essential for developing effective treatments for cardiac dysfunction.

Keywords:
G-protein-coupled receptorsGPCR kinasesbeta adrenoreceptorchronic heart failureextracellular receptor kinase1/2mitogen-activated protein kinaserenin-angiotensin-aldosterone system

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