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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Regulation of Membrane Targeting of the G Protein-coupled Receptor Kinase 2 by Protein Kinase A and Its Anchoring Protein AKAP79 [PDF]
Journal of Biological Chemistry, 2001 The beta 2 adrenergic receptor (beta 2AR) undergoes desensitization by a process involving its phosphorylation by both protein kinase A (PKA) and G protein-coupled receptor kinases (GRKs). The protein kinase A-anchoring protein AKAP79 influences beta 2AR
Chen, Wei +8 more
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G protein-coupled receptor kinase 2 (GRK2) as a multifunctional signaling hub. [PDF]
Cell Mol Life Sci, 2019 Accumulating evidence indicates that G protein-coupled receptor kinase 2 (GRK2) is a versatile protein that acts as a signaling hub by modulating G protein-coupled receptor (GPCR) signaling and also via phosphorylation or scaffolding interactions with an
Penela P +3 more
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Structures of rhodopsin in complex with G-protein-coupled receptor kinase 1. [PDF]
Nature, 2021 Chen Q +11 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 Kinase 3 Regulates Breast Cancer Migration, Invasion, and Metastasis. [PDF]
PLoS ONE, 2016 Triple negative breast cancer (TNBC) is a heterogeneous disease that has a poor prognosis and limited treatment options. Chemokine receptor interactions are important modulators of breast cancer metastasis; however, it is now recognized that quantitative
Matthew J Billard +13 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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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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