Historical Perspective of the G Protein-Coupled Receptor Kinase Family [PDF]
Cells, 2021 Agonist activation of G protein-coupled receptors promotes sequential interaction of the receptor with heterotrimeric G proteins, G protein-coupled receptor kinases (GRKs), and arrestins. GRKs play a central role in mediating the switch from G protein to
Jeffrey L. Benovic
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Aged G Protein-Coupled Receptor Kinase 3 (Grk3)-Deficient Mice Exhibit Enhanced Osteoclastogenesis and Develop Bone Lesions Analogous to Human Paget’s Disease of Bone [PDF]
Cells, 2023 Paget’s Disease of Bone (PDB) is a metabolic bone disease that is characterized by dysregulated osteoclast function leading to focal abnormalities of bone remodeling. It can lead to pain, fracture, and bone deformity. G protein-coupled receptor kinase 3 (
Emily M. Rabjohns +15 more
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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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Inhibition of thrombin receptor signaling by a G-protein coupled receptor kinase. Functional specificity among G-protein coupled receptor kinases. [PDF]
Journal of Biological Chemistry, 1994 The thrombin receptor, a member of the seven membrane-spanning superfamily of G-protein coupled receptors, is activated by an irreversible proteolytic mechanism, but signaling by activated thrombin receptors shuts off soon after receptor activation. This shut-off mechanism is thought to be required for concentration-dependent responses to thrombin and ...
Kenji Ishii +6 more
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Role of G-protein-coupled receptor kinase 4 on the dysfunction of renal Mas receptor in hypertension. [PDF]
PLoS ONEThe angiotensin converting enzyme 2/angiotensin-(1-7)/Mas receptor axis plays an important role in the regulation of blood pressure. G protein-coupled receptor kinase 4 (GRK4) has attracted more attentions by modulating G protein-coupled receptors and ...
Lin Chen +7 more
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G‐protein coupled receptor kinases as modulators of G‐protein signalling
The Journal of Physiology, 1999 G‐protein coupled receptors (GPCRs) comprise one of the largest classes of signalling molecules. A wide diversity of activating ligands induce the active conformation of GPCRs and lead to signalling via heterotrimeric G‐proteins and downstream effectors.
Moritz Bünemann, Marie Thérèse Hosey
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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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The Open Question of How GPCRs Interact with GPCR Kinases (GRKs)
Biomolecules, 2021 G protein-coupled receptors (GPCRs), which regulate a vast number of eukaryotic processes, are desensitized by various mechanisms but, most importantly, by the GPCR kinases (GRKs).
M. Claire Cato +6 more
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Targeting G protein–coupled receptor kinases to G protein–coupled receptors
Current Opinion in Endocrine and Metabolic Research, 2021 G protein-coupled receptors (GPCRs) interact with three protein families following agonist binding: heterotrimeric G proteins, G protein-coupled receptor kinases (GRKs) and arrestins. GRK-mediated phosphorylation of GPCRs promotes arrestin binding to uncouple the receptor from G protein, a process called desensitization, and for many GPCRs, arrestin ...
Jeffrey L. Benovic, Sarah M. Sulon
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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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