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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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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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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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Regulation of G Protein-Coupled Receptor Kinases by Phospholipids
Current Medicinal Chemistry, 2012G protein coupled-receptor (GPCR) kinases (GRKs) initiate the deactivation of GPCRs by phosphorylating their cytoplasmic loops and C-terminal tails. They are regulated not only by allosteric interactions with activated GPCRs, but also by the membrane environment itself.
K T, Homan, A, Glukhova, J J G, Tesmer
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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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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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Regulation of G Protein-Coupled Receptors by Receptor Kinases and Arrestins
1995Publisher Summary This chapter discusses the regulation of G protein-coupled receptors by receptor kinases and arrestins. Signal transduction through seven-transmembrane domain or serpentine receptors, which is mediated by guanine nucleotide-binding (G) proteins, accounts for a significant fraction of all signaling in the body.
R, Sterne-Marr, J L, Benovic
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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 Kinases and Hypertension
High Blood Pressure & Cardiovascular Prevention, 2006The understanding of molecular mechanisms of complex physiological phenomena, such as cardiac contractile function or blood pressure homeostasis, has generated the need for a new generation of scientists who must be able to conjugate intrinsic biological mechanisms and clinical manifestations of disease.
IACCARINO, Guido +4 more
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Regulation of G protein-coupled receptor kinase 2
2002Publisher Summary G protein-coupled receptor kinase 2 (GRK2) was originally termed a “β-adrenergic receptor kinase” (βARK) because it was purified as a kinase of the adrenergic β 2 receptor, and the adrenergic β 2 receptor was the only known substrate of GRK2. GRK2 is now known to phosphorylate different kinds of G protein-coupled receptors (GPCRs),
Tatsuya, Haga +4 more
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