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November 29, 2025Molecular PharmacologyOpen Access

GRK2 and GRK5—The 2 critical kinases in cardiac pathophysiology

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Why the study?

GRK2 and GRK5 are upregulated in heart failure across cardiac cell types, requiring examination of their cell-specific roles and therapeutic targeting.

Design

Review

Authors

RRRajika RoyDuke UniversityWalter J. KochWalter J. KochHeart Failure & Transplant

Discussion

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Implication

GRK2/GRK5 upregulation in HF may identify novel targets; leaves open cell-specific contributions in human disease.

Structured PICO

P
Population
Heart failure (human and mouse models)
I
Intervention
GRK2 and GRK5 inhibitors (e.g., paroxetine)

GRK2 and GRK5 play a central role in heart failure pathophysiology across multiple cardiac cell types, and their targeted inhibition represents a potential new therapeutic strategy.

Cite This Study

Roy et al. (2025) studied this question.

synapsesocial.com/papers/6a6f695235aa2c282ce0c6f4https://doi.org/10.1016/j.molpha.2025.100095

Topics

Heart failureHFrEF treatment
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Also Consider

Synapse has enriched 4 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Cardioprotective Effects of the GRK2 Inhibitor Paroxetine on Isoproterenol-Induced Cardiac Remodeling by Modulating NF-κB Mediated Prohypertrophic and Profibrotic Gene Expression2023 · 15 citations
  2. 2The role of G protein-coupled receptor kinase 4 in cardiomyocyte injury after myocardial infarction2020 · 50 citations
  3. 3Molecular Basis for Small Molecule Inhibition of G Protein-Coupled Receptor Kinases2014 · 58 citations
  4. 4The Metabolic Role of GRK2 in Insulin Resistance and Associated Conditions2021 · 30 citations