title: G-protein-coupled receptor kinase 2 and hypertension: molecular insights and pathophysiological mechanisms.
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.
authors.affiliation: Department of Advanced Biomedical Sciences, Federico II University of Naples, 80131, Naples, Italy. gaetano.santulli@unina.it
authors.forename: Gaetano
authors.initials: G
authors.lastname: Santulli
authors.forename: Bruno
authors.initials: B
authors.lastname: Trimarco
authors.forename: Guido
authors.initials: G
authors.lastname: Iaccarino
mesh_terms: D000818:Animals; D062186:Arterial Pressure; D004730:Endothelium, Vascular / Q000201:enzymology* / Q000503:physiopathology; D054769:G-Protein-Coupled Receptor Kinase 2 / Q000378:metabolism*; D006801:Humans; D006973:Hypertension / Q000201:enzymology* / Q000503:physiopathology; D011941:Receptors, Adrenergic / Q000378:metabolism*; D015398:Signal Transduction; D015854:Up-Regulation; D014664:Vasodilation
chemical_list: D011941:Receptors, Adrenergic; D054769:G-Protein-Coupled Receptor Kinase 2