Related Experiment Video

Updated: May 15, 2026

Mesenteric Artery Contraction and Relaxation Studies Using Automated Wire Myography
07:51

Mesenteric Artery Contraction and Relaxation Studies Using Automated Wire Myography

Published on: September 22, 2011

The role of G protein coupled receptor kinases in neurocardiovascular pathophysiology

Tijana Bojic1, Emina Sudar, Dimitri Mikhailidis

  • 1Institute of Nuclear Sciences Vinča, University of Belgrade, Laboratory of Radiobiology and Molecular Genetics, Belgrade, Serbia.

Archives of Medical Science : AMS
|January 16, 2013
PubMed

Insights

G protein-coupled receptor kinases (GRKs), particularly GRK-2, are implicated in heart failure following myocardial infarction. Lowering GRK-2 levels may reduce heart failure risk and indicate therapeutic efficacy in cardiovascular diseases.

Area of Science:

  • Cardiology
  • Molecular Biology
  • Biochemistry

Background:

  • G protein-coupled receptor kinases (GRKs) are involved in the desensitization of beta-adrenergic receptors (AR) following coronary occlusion.
  • Targeted deletion or reduction of cardiac myocyte GRK-2 has been shown to decrease the risk of post-ischemic heart failure (HF).
  • Human studies confirm GRK-2 as a marker for HF progression after myocardial infarction (MI).

Purpose of the Study:

  • To explore the role of GRKs in cardiovascular diseases, including heart failure and hypertension.
  • To investigate GRK-2 as a potential indicator of beta-AR blocker efficacy in acute coronary syndrome.
  • To understand the involvement of GRKs in the pathogenesis of neurocardiological disorders.

Main Methods:

  • Review of existing studies on GRK involvement in cardiovascular pathophysiology.
  • Analysis of human and animal model data regarding GRK levels in various cardiac conditions.
  • Exploration of the link between GRKs and therapeutic responses, such as beta-AR blocker efficacy.

Main Results:

  • Elevated GRK-2 levels are an early consequence of myocardial injury and are associated with HF progression.
  • Increased GRK-2 has been reported in hypertension in both animal models and humans.
  • GRK-2 levels may predict beta-AR blocker efficacy in acute coronary syndrome patients.

Conclusions:

  • GRK-2 plays a significant role in the pathophysiology of cardiovascular diseases like heart failure and hypertension.
  • GRK-2 serves as a potential biomarker for disease progression and therapeutic response.
  • Further research into GRKs could reveal new therapeutic strategies for neurocardiological diseases.
Keywords:
autonomicmolecular signaling pathwaysympatheticvagal

More Related Videos

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding10:13

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding

Published on: June 9, 2017

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators07:41

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

Published on: February 20, 2018

Related Concept Videos

G-Protein Gated Ion Channels01:21

G-Protein Gated Ion Channels

GPCRs are primarily responsible for our sense of smell, taste, and vision.  The binding of a sensory stimulus activates GPCR to stimulate effector proteins, many of which are ion channels in the sensory organs. GPCRs modulate the opening and closing of the target ion channels either directly by binding them, or by releasing second messengers that activate these channels. As ions move across the membrane, the membrane potential is altered, which induces an appropriate response.
Sensory organs,...
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
GPCR Desensitization01:12

GPCR Desensitization

G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
Interactions Between Signaling Pathways01:19

Interactions Between Signaling Pathways

Signaling cascades usually lack linearity. Multiple pathways interact and regulate one another, allowing cells to integrate and respond to diverse environmental stimuli.
Convergence and divergence, and cross-talk between signaling pathways
Two distinct signaling pathways can converge on a single functional unit, which may either be a single protein or a complex of proteins. The response is either functionally distinct or synergistic between the two pathways but different from the response...
GPCRs Regulate Adenylyl Cylase Activity01:09

GPCRs Regulate Adenylyl Cylase Activity

Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of cells.
Two...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.