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G-Protein-Coupled Receptor Kinase 2 and Hypertension

Molecular Insights and Pathophysiological Mechanisms

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Abstract

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.

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No sources of funding were used to assist in the preparation of this review. The authors have no conflicts of interest that are directly relevant to the content of this review.

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Authors and Affiliations

  1. Department of Advanced Biomedical Sciences, “Federico II” University of Naples, 80131, Naples, Italy

    Gaetano Santulli & Bruno Trimarco

  2. College of Physicians and Surgeons, Columbia University Medical Center, Manhattan, New York, NY, USA

    Gaetano Santulli

  3. Multimedica Research Hospital, Milan, Italy

    Guido Iaccarino

  4. Department of Medicine and Surgery, University of Salerno, Salerno, Italy

    Guido Iaccarino

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  1. Gaetano Santulli
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Correspondence to Gaetano Santulli.

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Santulli, G., Trimarco, B. & Iaccarino, G. G-Protein-Coupled Receptor Kinase 2 and Hypertension. High Blood Press Cardiovasc Prev 20, 5–12 (2013). https://doi.org/10.1007/s40292-013-0001-8

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