G Protein-Coupled Receptor Kinase 2 as Novel Therapeutic Target in Fibrotic Diseases [PDF]
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
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G protein-coupled receptor kinase-2 (GRK-2) controls exploration through neuropeptide signaling in Caenorhabditis elegans. [PDF]
PLoS Genetics, 2023 Animals alter their behavior in manners that depend on environmental conditions as well as their developmental and metabolic states. For example, C. elegans is quiescent during larval molts or during conditions of satiety.
Kristen Davis +6 more
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Dopamine-induced arrestin recruitment and desensitization of the dopamine D4 receptor is regulated by G protein-coupled receptor kinase-2 [PDF]
Frontiers in Pharmacology, 2023 The dopamine D4 receptor (D4R) is expressed in the retina, prefrontal cortex, and autonomic nervous system and has been implicated in attention deficit hyperactivity disorder (ADHD), substance use disorders, and erectile dysfunction.
Viktor Burström +11 more
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G protein-coupled receptor kinase 2 promotes cardiac hypertrophy. [PDF]
PLoS ONE, 2017 The increase in protein activity and upregulation of G-protein coupled receptor kinase 2 (GRK2) is a hallmark of cardiac stress and heart failure. Inhibition of GRK2 improved cardiac function and survival and diminished cardiac remodeling in various ...
Philipp Schlegel +12 more
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The Regulator of G Protein Signaling Homologous Domain of G Protein-Coupled Receptor Kinase 2 Mediates Short-Term Desensitization of β3-Adrenergic Receptor [PDF]
Frontiers in Pharmacology, 2020 G protein coupled receptor (GPCR) kinases (GRKs) are key regulators of GPCR signaling. Canonical mechanism of GPCR desensitization involves receptor phosphorylation by GRKs followed by arrestin recruitment and uncoupling from heterotrimeric G protein ...
Emiliana Echeverría +18 more
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Regulation of G protein-coupled receptor kinase 2 and its role in tumors [PDF]
Journal of Translational MedicineBackground G protein-coupled receptor kinase 2(GRK2) is a pivotal regulator of G protein-coupled receptor (GPCR) signal desensitization. It is increasingly recognized for its involvement in the pathogenesis of various malignancies through non-canonical ...
Chenmin Liu +4 more
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Aldosterone Jeopardizes Myocardial Insulin and β-Adrenergic Receptor Signaling via G Protein-Coupled Receptor Kinase 2 [PDF]
Frontiers in Pharmacology, 2019 Hyperaldosteronism alters cardiac function, inducing adverse left ventricle (LV) remodeling either via increased fibrosis deposition, mitochondrial dysfunction, or both.
Alessandro Cannavo +16 more
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G-Protein-Coupled Receptor Kinase 2 Limits CCL21-Induced T Cell Migration via Phospholipase Cγ1 [PDF]
ReceptorsBackground/Objectives: G protein-coupled receptors (GPCRs) can promote ligand-biased signaling, yet the mechanisms that promote bias are not well understood.
Anahi Sanchez +14 more
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G Protein-Coupled Receptor Kinase 2 Selectively Enhances β-Arrestin Recruitment to the D2 Dopamine Receptor through Mechanisms That Are Independent of Receptor Phosphorylation [PDF]
Biomolecules, 2023 The D2 dopamine receptor (D2R) signals through both G proteins and β-arrestins to regulate important physiological processes, such as movement, reward circuitry, emotion, and cognition.
Marta Sánchez-Soto +12 more
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G Protein-Coupled Receptor Kinase 2 (GRK2) as a Potential Therapeutic Target in Cardiovascular and Metabolic Diseases [PDF]
Frontiers in Pharmacology, 2019 G protein-coupled receptor kinase 2 (GRK2) is a central signaling node involved in the modulation of many G protein-coupled receptors (GPCRs) and also displaying regulatory functions in other cell signaling routes.
Cristina Murga +17 more
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