Document Detail

Regulation of GPCR signaling in hypertension.
MedLine Citation:
PMID:  20060896     Owner:  NLM     Status:  MEDLINE    
Hypertension represents a complex, multifactorial disease and contributes to the major causes of morbidity and mortality in industrialized countries: ischemic and hypertensive heart disease, stroke, peripheral atherosclerosis and renal failure. Current pharmacological therapy of essential hypertension focuses on the regulation of vascular resistance by inhibition of hormones such as catecholamines and angiotensin II, blocking them from receptor activation. Interaction of G-protein coupled receptor kinases (GRKs) and regulator of G-protein signaling (RGS) proteins with activated G-protein coupled receptors (GPCRs) effect the phosphorylation state of the receptor leading to desensitization and can profoundly impair signaling. Defects in GPCR regulation via these modulators have severe consequences affecting GPCR-stimulated biological responses in pathological situations such as hypertension, since they fine-tune and balance the major transmitters of vessel constriction versus dilatation, thus representing valuable new targets for anti-hypertensive therapeutic strategies. Elevated levels of GRKs are associated with human hypertensive disease and are relevant modulators of blood pressure in animal models of hypertension. This implies therapeutic perspective in a disease that has a prevalence of 65million in the United States while being directly correlated with occurrence of major adverse cardiac and vascular events. Therefore, therapeutic approaches using the inhibition of GRKs to regulate GPCRs are intriguing novel targets for treatment of hypertension and heart failure.
Henriette L Brinks; Andrea D Eckhart
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Review     Date:  2010-01-11
Journal Detail:
Title:  Biochimica et biophysica acta     Volume:  1802     ISSN:  0006-3002     ISO Abbreviation:  Biochim. Biophys. Acta     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-11-01     Completed Date:  2010-12-21     Revised Date:  2014-09-18    
Medline Journal Info:
Nlm Unique ID:  0217513     Medline TA:  Biochim Biophys Acta     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  1268-75     Citation Subset:  IM    
Copyright Information:
Copyright © 2010 Elsevier B.V. All rights reserved.
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MeSH Terms
Angiotensin II / genetics,  metabolism
Antihypertensive Agents / therapeutic use
Blood Pressure / genetics
Catecholamines / genetics,  metabolism
Disease Models, Animal
GTP-Binding Proteins / genetics,  metabolism
Hypertension / drug therapy,  epidemiology,  genetics,  metabolism*
Receptor Protein-Tyrosine Kinases / genetics,  metabolism
Receptors, G-Protein-Coupled / genetics,  metabolism*
Signal Transduction*
United States / epidemiology
Vasoconstriction / genetics
Vasodilation / genetics
Grant Support
P01 HL091799/HL/NHLBI NIH HHS; P01 HL091799-019002/HL/NHLBI NIH HHS; P01 HL091799-035662/HL/NHLBI NIH HHS; R01 HL069847/HL/NHLBI NIH HHS; R01 HL069847-01A2/HL/NHLBI NIH HHS
Reg. No./Substance:
0/Antihypertensive Agents; 0/Catecholamines; 0/Receptors, G-Protein-Coupled; 11128-99-7/Angiotensin II; EC Protein-Tyrosine Kinases; EC 3.6.1.-/GTP-Binding Proteins

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