GRK2, G protein-coupled receptor kinase 2, 156

N. diseases: 159; N. variants: 2
Source: ALL
Disease Score gda Association Type Type Original DB Sentence supporting the association PMID PMID Year
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
Heart failure
0.600 Biomarker disease BEFREE Higher βARK1 is associated with worse physical HF symptoms, pinpointing a potential pathophysiologic underpinning. 29803296 2019
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
Heart failure
0.600 Biomarker disease BEFREE Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. 28699740 2017
CUI: C0018801
Disease: Heart failure
Heart failure
0.600 Biomarker disease BEFREE More consistent to mammalians, adult zebrafish developed significant heart failure in concert with β1-AR downregulation, and GRK2 and brain natriuretic peptide (BNP) upregulation in response to prolonged, 14d ISO-stimulation. 28554511 2017
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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
CUI: C0018801
Disease: Heart failure
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