The GRK2/AP‐1 Signaling Axis Mediates Vascular Endothelial Dysfunction and Atherosclerosis Induced by Oscillatory Low Shear Stress
Sign Up to like & getrecommendations! Published in 2025 at "Advanced Science"
DOI: 10.1002/advs.202501981
Abstract: Disturbed blood flow and the resulting oscillatory low shear stress (OSS) are key contributors to vascular endothelial dysfunction and the initiation of atherosclerosis. However, the molecular mediators that translate abnormal hemodynamic signals into pathological vascular… read more here.
Keywords: vascular endothelial; grk2; atherosclerosis; endothelial dysfunction ... See more keywords
Cell therapy rescues aging-induced beta-1 adrenergic receptor and GRK2 dysfunction in the coronary microcirculation.
Sign Up to like & getrecommendations! Published in 2021 at "GeroScience"
DOI: 10.1007/s11357-021-00455-6
Abstract: Our past study showed that coronary arterioles isolated from adipose-derived stromal vascular fraction (SVF)-treated rats showed amelioration of the age-related decrease in vasodilation to beta-adrenergic receptor (β-AR) agonist and improved β-AR-dependent coronary flow and microvascular… read more here.
Keywords: vasodilation; grk2; svf; receptor ... See more keywords
G protein-coupled receptor kinase 2 contributes to impaired fatty acid metabolism in the failing heart.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of molecular and cellular cardiology"
DOI: 10.1016/j.yjmcc.2018.08.025
Abstract: Increased G protein-coupled receptor kinase (GRK)2 is central to heart failure (HF) pathogenesis, via desensitization of β-adrenergic receptors and loss of contractile reserve. Since GRK2 has been shown to compromise fatty acid (FA) oxidation, this… read more here.
Keywords: heart; kinase; grk2; protein coupled ... See more keywords
A peptide of the amino-terminus of GRK2 induces hypertrophy and yet elicits cardioprotection after pressure overload.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of molecular and cellular cardiology"
DOI: 10.1016/j.yjmcc.2021.01.004
Abstract: G protein-coupled receptor (GPCR) kinase 2 (GRK2) expression and activity are elevated early on in response to several forms of cardiovascular stress and are a hallmark of heart failure. Interestingly, though, in addition to its… read more here.
Keywords: arknt mice; stress; pressure overload; grk2 ... See more keywords
GRK2 Dictates a Functional Switch of the Peripheral Mu-Opioid Receptor.
Sign Up to like & getrecommendations! Published in 2020 at "ACS chemical neuroscience"
DOI: 10.1021/acschemneuro.0c00622
Abstract: The peripheral mu-opioid receptor (MOR) has been recognized as a potential target to provide safer analgesia with reduced central side effects. Although analgesic incompetence of the peripheral MOR in the absence of inflammation was initially… read more here.
Keywords: peripheral opioid; opioid receptor; mor; kinase ... See more keywords
Is GRK2 a new target for cardiovascular disease?
Sign Up to like & getrecommendations! Published in 2018 at "Hypertension Research"
DOI: 10.1038/s41440-018-0052-2
Abstract: Recently, many reports have indicated that G protein, G protein-coupled receptors (GPCR), and related enzymes play an important role in cardiovascular disease. GPCR are also known as seven-(pass)-transmembrane domain receptors that are coupled with G… read more here.
Keywords: protein; insulin; grk2; target ... See more keywords
GRK2 contributes to glucose mediated calcium responses and insulin secretion in pancreatic islet cells
Sign Up to like & getrecommendations! Published in 2021 at "Scientific Reports"
DOI: 10.1038/s41598-021-90253-z
Abstract: Diabetes is a metabolic syndrome rooted in impaired insulin and/or glucagon secretory responses within the pancreatic islets of Langerhans (islets). Insulin secretion is primarily regulated by two key factors: glucose-mediated ATP production and G-protein coupled… read more here.
Keywords: secretion; insulin secretion; glucose mediated; grk2 ... See more keywords
GRK specificity and Gβγ dependency determines the potential of a GPCR for arrestin-biased agonism
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DOI: 10.1038/s42003-024-06490-1
Abstract: G protein-coupled receptors (GPCRs) are mainly regulated by GPCR kinase (GRK) phosphorylation and subsequent β-arrestin recruitment. The ubiquitously expressed GRKs are classified into cytosolic GRK2/3 and membrane-tethered GRK5/6 subfamilies. GRK2/3 interact with activated G protein… read more here.
Keywords: grk2; biased agonism; arrestin biased; grk specificity ... See more keywords
GRK2–YAP signaling is implicated in pulmonary arterial hypertension development
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DOI: 10.1097/cm9.0000000000002946
Abstract: Abstract Background: Pulmonary arterial hypertension (PAH) is characterized by excessive proliferation of small pulmonary arterial vascular smooth muscle cells (PASMCs), endothelial dysfunction, and extracellular matrix remodeling. G protein-coupled receptor kinase 2 (GRK2) plays an important… read more here.
Keywords: mice; grk2; yap; expression ... See more keywords
GRK2 kinases in the primary cilium initiate SMOOTHENED-PKA signaling in the Hedgehog cascade
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DOI: 10.1124/jpet.553.951480
Abstract: During Hedgehog (Hh) signal transduction in development and disease, the atypical G protein-coupled receptor (GPCR) SMOOTHENED (SMO) communicates with GLI transcription factors by binding the protein kinase A catalytic subunit (PKA-C) and physically blocking its… read more here.
Keywords: grk2; grk2 kinases; kinases primary; primary cilium ... See more keywords
Abstract 4369579: Loss of G Protein-Coupled Receptor Kinase 2 S-Nitrosylation Abolishes Beta 3 Adrenergic Receptor-Mediated Cardioprotection Evidence from Functional and Proteomic Analyses
Sign Up to like & getrecommendations! Published in 2025 at "Circulation"
DOI: 10.1161/circ.152.suppl_3.4369579
Abstract: Background: G Protein-Coupled Receptor Kinase 2 (GRK2) contributes to cardiac dysfunction through β-Adrenoceptor (βAR) desensitization following its upregulation. Inhibition of GRK2 has been shown to improve cardiac function. Nitric oxide (NO), through the formation of… read more here.
Keywords: receptor; mice; grk2; protein coupled ... See more keywords