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G-protein-coupled receptor regulation: role of G-protein-coupled receptor kinases and arrestins
Canadian Journal of Physiology and Pharmacology, 1996G-protein-coupled receptors (GPCRs) represent a large family of proteins that transduce extracellular signals to the interior of cells. Signalling through these receptors rapidly desensitized primarily as the consequence of receptor phosphorylation, but receptor sequestration and downregulation can also contribute to this process.
S S, Ferguson +3 more
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G Protein Coupled Receptor Kinases
2007G protein-coupled receptor kinases (GRKs) belong to the AGC family of serine/threonine kinases. They phosphorylate agonist-activated G protein-coupled receptors (hence the name). This phosphorylation triggers the binding of arrestins to the receptors.
Cornelius Krasel, Martin J. Lohse
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Characterization of G protein-coupled receptor kinases
2002Publisher Summary A basic feature of most cells is the ability to dynamically regulate their responsiveness to extracellular stimuli. Numerous stimuli transmit their signals via interaction with cell surface G protein-coupled receptors (GPCRs). GPCRs are subject to three principal modes of regulation: (1) desensitization, the process by which a ...
Alexey N, Pronin +2 more
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G Protein-Coupled Receptor Kinases
2005As the largest family of membrane receptors, G protein-coupled receptors (GPCRs) transduce a large number of extracellular signals from hormones, neurotransmitters, chemokines, and other environmental stimuli to the interior of cells and play fundamental roles in the regulation of cellular functions.
Lan Ma, Jingxia Gao, Xiaoqing Chen
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Tyrosine Kinase Receptor Transactivation Associated to G Protein- Coupled Receptors
Current Drug Targets, 2010G protein-coupled receptors (GPCRs) comprise a large family of membrane receptors involved in signal transduction. These receptors are linked to a variety of physiological and biological processes such as regulation of neurotransmission, growth, cell differentiation and oncogenesis among others.
Vanessa, Almendro +2 more
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G-Protein–coupled receptor kinase expression in hypertension
Clinical Pharmacology & Therapeutics, 1999In human hypertension we have recently identified an increase in lymphocyte G-protein receptor kinase-2 (GRK-2) protein expression, the key protein regulating the interaction between G-protein-coupled receptors and activation of adenylyl cyclase. However, it was not known whether this increase in GRK-2 protein expression was attributable to regulation ...
R, Gros +5 more
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Pathophysiological roles of G-protein-coupled receptor kinases
Cellular Signalling, 2005G-protein-coupled receptor kinases (GRKs) interact with the agonist-activated form of G-protein-coupled receptors (GPCRs) to effect receptor phosphorylation and to initiate profound impairment of receptor signalling, or desensitization. GPCRs form the largest family of cell surface receptors known and defects in GRK function have the potential ...
Thierry, Métayé +3 more
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Peptide inhibitors of G protein-coupled receptor kinases
Biochemical Pharmacology, 2005G protein-coupled receptor kinases (GRKs) are regulatory enzymes involved in the modulation of seven-transmembrane-helix receptors. In order to develop specific inhibitors for these kinases, we synthesized and investigated peptide inhibitors derived from the sequence of the first intracellular loop of the beta2-adrenergic receptor.
Rainer, Winstel +4 more
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Targeting G protein-coupled receptor kinases to their receptor substrates
Journal of Membrane Biology, 1997Membrane association is essential for GRK function and because of this the GRKs have evolved complex regulatory mechanisms for associating with the membrane. Although the GRKs are highly homologous, each kinase utilizes a distinct mechanism for associating with the membrane, which makes it unique within the family.
R H, Stoffel +2 more
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G-protein-coupled receptor kinases and the heart
Trends in Cardiovascular Medicine, 1995The family of G-protein-coupled receptors includes many well-studied members, such as the adrenergic and the muscarinic acetylcholine receptors. These receptors are regulated by multiple mechanisms that serve to adapt their expression and their function to a rapidly changing environment.
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