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

Authors:
Gaetano Santulli
Gaetano Santulli
Federico II University of Naples
Italy
Bruno Trimarco
Bruno Trimarco
Federico II University
Napoli | Italy
Prof. Guido Iaccarino, MD, PhD
Prof. Guido Iaccarino, MD, PhD
Federico II University of Naples
Full Professor of Applied Medical Science and Technology
Cardiology
Napoli, Campania | Italy

High Blood Press Cardiovasc Prev 2013 Mar 27;20(1):5-12. Epub 2013 Mar 27.

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

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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http://dx.doi.org/10.1007/s40292-013-0001-8DOI Listing
March 2013
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46 Citations

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