G-protein-coupled receptor kinase 2 and hypertension: Molecular insights and pathophysiological mechanisms

Gaetano Santulli, Bruno Trimarco, Guido Iaccarino

Research output: Contribution to journalReview articlepeer-review

98 Scopus citations


Numerous factors partake in the fine-tuning of arterial blood pressure. The heptahelical G-protein-coupled receptors (GPCRs) represent one of the largest classes of cell-surface receptors. Further, ligands directed at GPCRs account for nearly 30 % of current clinical pharmaceutical agents available. Given the wide variety of GPCRs involved in blood pressure control, it is reasonable to speculate for a potential role of established intermediaries involved in the GPCR desensitization process, like the G-protein-coupled receptor kinases (GRKs), in the regulation of vascular tone. Of the seven mammalian GRKs, GRK2 seems to be the most relevant isoform at the cardiovascular level. This review attempts to assemble the currently available information concerning GRK2 and hypertension, opening new potential fields of translational investigation to treat this vexing disease.

Original languageEnglish (US)
Pages (from-to)5-12
Number of pages8
JournalHigh Blood Pressure and Cardiovascular Prevention
Issue number1
StatePublished - Mar 2013
Externally publishedYes


  • Adrenergic receptors
  • Endothelium
  • GRK
  • Hypertension
  • Vascular tone

ASJC Scopus subject areas

  • Internal Medicine
  • Cardiology and Cardiovascular Medicine


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