Inhibition of G-protein-coupled receptor kinase 2 (GRK2) triggers the growth-promoting mitogen-activated protein kinase (MAPK) pathway. [PDF]
J Biol Chem, 2013 Inhibition of G-protein-coupled receptor kinase 2 (GRK2) is an emerging treatment option for heart failure. Because GRK2 is also indispensable for growth and development, we analyzed the impact of GRK2 inhibition on cell growth and proliferation. Inhibition of GRK2 by the dominant-negative GRK2-K220R did not affect the proliferation of cultured cells ...
Fu X, Koller S, Abd Alla J, Quitterer U.
europepmc +7 more sources
G Protein-Coupled Receptor Kinase 2 as Novel Therapeutic Target in Fibrotic Diseases
Frontiers in Immunology, 2022 G protein-coupled receptor kinase 2 (GRK2), an important subtype of GRKs, specifically phosphorylates agonist-activated G protein-coupled receptors (GPCRs).
Nan Li +9 more
doaj +1 more source
Clathrin Required for Phosphorylation and Internalization of β2-Adrenergic Receptor by G Protein-coupled Receptor Kinase 2 (GRK2) [PDF]
Journal of Biological Chemistry, 2006 Clathrin is a major component of clathrin-coated pits and serves as a binding scaffold for endocytic machinery through the binding of a specific sequence known as the clathrin-binding motif. This motif is also found in cellular signaling proteins other than endocytic components, including G protein-coupled receptor kinase 2 (GRK2), which phosphorylates
Supachoke, Mangmool +6 more
openaire +2 more sources
Potential Regulatory Roles of GRK2 in Endothelial Cell Activity and Pathological Angiogenesis
Frontiers in Immunology, 2021 G protein-coupled receptor (GPCR) kinase 2 (GRK2) is an integrative node in many signaling network cascades. Emerging evidence indicates that GRK2 can interact with a large number of GPCRs and non-GPCR substrates in both kinase-dependent and -independent
Jiajie Kuai, Chenchen Han, Wei Wei
doaj +1 more source
Tailoring therapy for heart failure: the pharmacogenomics of adrenergic receptor signaling. [PDF]
, 2014 Heart failure is one of the leading causes of mortality in Western countries, and β-blockers are a cornerstone of its treatment. However, the response to these drugs is variable among individuals, which might be explained, at least in part, by genetic ...
Barrese, V +3 more
core +2 more sources
GRK2 differentially regulates FcεRI and MRGPRB2-mediated responses in mast cells
Frontiers in Immunology, 2023 In addition to high-affinity IgE receptor (FcεRI), a subtype of mouse mast cells (MCs) expresses a G protein-coupled receptor known as Mas-related G protein-coupled receptor (GPCR)-B2 (MRGPRB2; human ortholog MRGPRX2).
Monica Thapaliya, Hydar Ali
doaj +1 more source
G protein-coupled receptor kinase-2 (GRK-2) regulates serotonin metabolism through the monoamine oxidase AMX-2 in Caenorhabditis elegans. [PDF]
, 2017 G protein-coupled receptors (GPCRs) regulate many animal behaviors. GPCR signaling is mediated by agonist-promoted interactions of GPCRs with heterotrimeric G proteins, GPCR kinases (GRKs), and arrestins.
Aryal, Dipendra K. +5 more
core +2 more sources
G Protein-coupled receptor kinase 2 (GRK2): A novel modulator of insulin resistance
Archives of Physiology and Biochemistry, 2011 G protein-coupled receptor kinase 2 (GRK2) is emerging as a key, integrative node in many signalling pathways. Besides its canonical role in the modulation of the signalling mediated by many G protein-coupled receptors (GPCR), this protein can display a very complex network of functional interactions with a variety of signal transduction partners, in a
Mayor Menéndez, Federico +7 more
openaire +3 more sources
Feedback Inhibition of G Protein-coupled Receptor Kinase 2 (GRK2) Activity by Extracellular Signal-regulated Kinases [PDF]
Journal of Biological Chemistry, 1999 G protein-coupled receptor kinase (GRK)-mediated receptor phosphorylation and beta-arrestin binding uncouple G protein-coupled receptors (GPCRs) from their respective G proteins and initiates the process of receptor internalization. In the case of the beta(2)-adrenergic receptor and lysophosphatidic acid receptor, these processes can lead to ERK ...
J A, Pitcher +5 more
openaire +2 more sources
A novel GRK2/HDAC6 interaction modulates cell spreading and motility [PDF]
, 2011 Cell motility and adhesion involves dynamic microtubule (MT) acetylation/deacetylation, a process regulated by enzymes as HDAC6, a major cytoplasmic α-tubulin deacetylase.
Aymerich, Ivette +4 more
core +2 more sources