TY - JOUR
T1 - G-protein-coupled receptor kinase 2 and hypertension
T2 - Molecular insights and pathophysiological mechanisms
AU - Santulli, Gaetano
AU - Trimarco, Bruno
AU - Iaccarino, Guido
PY - 2013/3
Y1 - 2013/3
N2 - 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.
AB - 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.
KW - Adrenergic receptors
KW - Endothelium
KW - GRK
KW - Hypertension
KW - Vascular tone
UR - http://www.scopus.com/inward/record.url?scp=84879391693&partnerID=8YFLogxK
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U2 - 10.1007/s40292-013-0001-8
DO - 10.1007/s40292-013-0001-8
M3 - Article
C2 - 23532739
AN - SCOPUS:84879391693
SN - 1120-9879
VL - 20
SP - 5
EP - 12
JO - High Blood Pressure and Cardiovascular Prevention
JF - High Blood Pressure and Cardiovascular Prevention
IS - 1
ER -