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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |