Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
Moreover, the pathological involvement of Angiotensin-converting enzyme 1 (ACE1)/angiotensin II (Ang II)/angiotensin II type 1 (AT1) axis and beneficial ACE2/Ang (1-7)/Mas receptor axis also shows protective role via Gi βγ, during heart failure these receptors get desensitized or internalized due to increase in the activity of G-protein-coupled receptor kinase 2 (GRK2) and GRK5, responsible for phosphorylation of G-protein-mediated down regulatory signaling.
|
31785110 |
2020 |
Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
GRK2 levels and activity have been reported to be enhanced in patients or in preclinical models of several relevant pathological situations, such as heart failure, cardiac hypertrophy, hypertension, obesity and insulin resistance conditions, or non-alcoholic fatty liver disease (NAFLD), and to contribute to disease progression by a variety of mechanisms related to its multifunctional roles.
|
30837878 |
2019 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
It has been shown that lowering cardiac G-protein-coupled-receptor-kinase-2 (GRK2) activity with βARKct expression, a peptide inhibitor of protein-coupled-receptor-kinase-2 (GRK2), results in improvement of heart failure in several different animal models.
|
30782477 |
2019 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Higher βARK1 is associated with worse physical HF symptoms, pinpointing a potential pathophysiologic underpinning.
|
29803296 |
2019 |
Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
The gene expression pattern of GRK2 and β2-adrenoceptor as molecular markers of cardiac dysfunction was altered in patients with severe PR compared with controls and was similar to expression in patients with advanced HF.
|
30104167 |
2019 |
Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
Given that increased expression and activity of GRK2 and GRK5 contribute to the loss of contractile reserve in the stressed and failing heart, inhibition of overactive GRKs has been proposed as a novel therapeutic approach to treat heart failure.
|
31186538 |
2019 |
Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
The expression of G protein-coupled receptor kinase 2 (GRK2), a key signaling hub, is up-regulated in the long-term in patients and in experimental models of heart failure.
|
31594751 |
2019 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Among them, GRK2 has been described to be upregulated in many pathological conditions and its crucial role in cardiac hypertrophy, hypertension, and heart failure promoted the search for pharmacological inhibitors of its activity.
|
31525427 |
2019 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
This study may be used in designing more potent and selective GRK2 inhibitors for therapeutic intervention of heart failure.
|
31506468 |
2019 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
A vast body of literature has established GRK2 as a key player in the development and progression of heart failure.
|
30946029 |
2019 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Since GRK2 has been shown to compromise fatty acid (FA) oxidation, this kinase may link metabolic and contractile defects in HF.
|
30171848 |
2018 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Last, we will update the readers on the current status of GRK2 inhibitors as a potential therapeutic strategy for heart failure with an emphasis on their ability of rescuing NO bioavailability.
|
28077324 |
2018 |
Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
The G-protein-coupled receptor kinase 2 (GRK2) plays a major role in cardiovascular diseases, and its expression is increased in heart failure.
|
29905975 |
2018 |
Congestive heart failure
|
0.600 |
GeneticVariation
|
disease |
BEFREE |
Thus, sensitization of the heart failure-promoting AT1 receptor by the RKIP-GRK2 interaction contributes to heart failure whereas dominant-negative GRK2-K220R is cardioprotective.
|
30687708 |
2018 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
In animal models, GRK2 contributes to the pathogenesis of heart failure after ischemia-reperfusion (IR) injury.
|
30538174 |
2018 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
(-)-Epigallocatechin-3-gallate, the major green tea catechin, regulates the desensitization of β1 adrenoceptor via GRK2 in experimental heart failure.
|
29247373 |
2018 |
Congestive heart failure
|
0.600 |
Therapeutic
|
disease |
RGD |
(-)-Epigallocatechin-3-gallate, the major green tea catechin, regulates the desensitization of β1 adrenoceptor via GRK2 in experimental heart failure.
|
29247373 |
2018 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Herein, we will update the readers about the 'state-of-art' of GRK2 inhibition as a potent therapeutic strategy in HF.
|
29166798 |
2018 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
The increase in protein activity and upregulation of G-protein coupled receptor kinase 2 (GRK2) is a hallmark of cardiac stress and heart failure.
|
28759639 |
2017 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
LVAD treatment in children with heart failure results in reversal of several pathologic myocellular processes, and G protein-coupled receptor kinase-2 may regulate β<sub>1</sub>-AR but not β<sub>2</sub>-adrenergic receptor expression in children with heart failure.
|
27908653 |
2017 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Small molecule Gβγ-GRK2 inhibition initiated 1 week post-injury was cardioprotective in the I/R model of chronic HF, including preservation of cardiac contractility and a reduction in cardiac fibrotic remodeling.
|
28818206 |
2017 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
This review summarizes what is currently known regarding the activity of these kinases, and particularly the role of GRK2 and GRK5 in the molecular alterations that occur during heart failure.
|
28328744 |
2017 |
Congestive heart failure
|
0.600 |
AlteredExpression
|
disease |
BEFREE |
In addition, chronic overexpression of GRK2 inhibits catecholamine induction of vital positive chronotropic and ionotropic effects required to preserve cardiac output leading to worsening of congestive HF.
|
27222484 |
2017 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
These studies elucidate a novel mechanism by which hyperinsulinemia contributes to heart failure by increasing PDE4D expression and identify β<sub>2</sub>AR or GRK2 as plausible therapeutic targets for preventing or treating heart failure in subjects with type 2 DM.
|
27815373 |
2017 |
Congestive heart failure
|
0.600 |
Biomarker
|
disease |
BEFREE |
Increased Atrial β-Adrenergic Receptors and GRK-2 Gene Expression Can Play a Fundamental Role in Heart Failure After Repair of Congenital Heart Disease with Cardiopulmonary Bypass.
|
28214967 |
2017 |