Search results for "G protein-coupled receptor kinase"

showing 10 items of 14 documents

The Amino-Terminal Domain of GRK5 Inhibits Cardiac Hypertrophy through the Regulation of Calcium-Calmodulin Dependent Transcription Factors.

2018

We have recently demonstrated that the amino-terminal domain of G protein coupled receptor kinase (GRK) type 5, (GRK5-NT) inhibits NFκB activity in cardiac cells leading to a significant amelioration of LVH. Since GRK5-NT is known to bind calmodulin, this study aimed to evaluate the functional role of GRK5-NT in the regulation of calcium-calmodulin-dependent transcription factors. We found that the overexpression of GRK5-NT in cardiomyoblasts significantly reduced the activation and the nuclear translocation of NFAT and its cofactor GATA-4 in response to phenylephrine (PE). These results were confirmed in vivo in spontaneously hypertensive rats (SHR), in which intramyocardial adenovirus-med…

0301 basic medicineG-Protein-Coupled Receptor Kinase 5MalecalmodulinMutantWistarPlasma protein binding030204 cardiovascular system & hematologyCatalysilcsh:ChemistryPhenylephrine0302 clinical medicineRats Inbred SHRMyocytes Cardiaclcsh:QH301-705.5SpectroscopybiologyChemistrycardiac hypertrophyNFATComputer Science Applications1707 Computer Vision and Pattern RecognitionGeneral MedicineLeft VentricularComputer Science ApplicationsCell biologycardiac hypertrophy; transcription factors; calmodulin; GRKGRKHypertrophy Left VentricularCardiacProtein BindingInbred SHRCalmodulinCalmodulin; Cardiac hypertrophy; GRK; Transcription factors; Animals; Binding Sites; Calmodulin; Cell Line; G-Protein-Coupled Receptor Kinase 5; GATA4 Transcription Factor; Hypertrophy Left Ventricular; Male; Myocytes Cardiac; NFATC Transcription Factors; Phenylephrine; Protein Binding; Rats; Rats Inbred SHR; Rats Wistar; Catalysis; Molecular Biology; Spectroscopy; Computer Science Applications1707 Computer Vision and Pattern Recognition; Physical and Theoretical Chemistry; Organic Chemistry; Inorganic ChemistryCatalysisArticleCell LineInorganic Chemistry03 medical and health sciencesG-Protein-Coupled Receptor Kinase 5transcription factorsAnimalsPhysical and Theoretical ChemistryRats WistarTranscription factorMolecular BiologyG protein-coupled receptor kinaseMyocytesBinding SitesNFATC Transcription FactorsOrganic ChemistryHypertrophyNFATC Transcription FactorsGATA4 Transcription FactorRats030104 developmental biologylcsh:Biology (General)lcsh:QD1-999biology.proteinTranscription factorInternational journal of molecular sciences
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Myocardial and Peripheral Lymphocytic Transcriptomic Dissociation of β-adrenoceptors and G Protein–coupled Receptor Kinases in Heart Transplantation

2009

Background The genetic expression of adrenergic receptors plays an important pathophysiologic role in heart failure. G protein–coupled receptor kinases (GRKs) desensitize the β-receptor to catecholaminergic stimulation. It has been suggested that their mRNA expression in peripheral lymphocytes could mirror the changes in their myocardial expression in the failing heart, but this relationship between the myocyte and lymphocyte has not been studied in heart transplantation (HT). The objective of this study was to analyze adrenergic receptor and GRK mRNA expression in myocardium and lymphocytes and their correlation. Methods Twenty-three HT patients without evidence of acute rejection or echoc…

AdultPulmonary and Respiratory Medicinemedicine.medical_specialtyAdrenergic receptorBiopsymedicine.medical_treatmentLymphocyteInternal medicineReceptors Adrenergic betamedicineHumansLymphocytesRNA MessengerReceptorHeart transplantationTransplantationG protein-coupled receptor kinasebiologybusiness.industryGene Expression ProfilingMyocardiumBeta adrenergic receptor kinaseHeartMiddle AgedG-Protein-Coupled Receptor Kinasesmedicine.diseaseTransplantationEndocrinologymedicine.anatomical_structureHeart failurebiology.proteinHeart TransplantationSurgeryReceptors Adrenergic beta-2Receptors Adrenergic beta-1Cardiology and Cardiovascular MedicinebusinessThe Journal of Heart and Lung Transplantation
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Changes in Adrenoceptors and G-Protein-Coupled Receptor Kinase 2 in <smlcap>L</smlcap>-NAME-Induced Hypertension Compared to Spontaneous …

2014

This work compares the expression of adrenoceptors (ARs) and G-protein-coupled receptor kinase (GRK) 2 (RT-PCR and immunoblotting) and functional responses in conductance (aorta) and resistance vessels (mesenteric resistance arteries; MRA) in two different models of rat hypertension: hypertension induced by chronic treatment with <smlcap>L</smlcap>-NAME (N<sup>G</sup>-nitro-<smlcap>L</smlcap>-arginine methyl-ester) (<smlcap>L</smlcap>-NAME-treated rats; LNHR), and genetically induced hypertension (spontaneously hypertensive rats; SHR). Changes found in the aorta, but not in the MRA, were: (1) a loss of contractile capacity, more evidently in α…

Aortamedicine.medical_specialtyG protein-coupled receptor kinaseContraction (grammar)biologyAdrenergic receptorPhysiologybusiness.industryBeta adrenergic receptor kinaseVasodilationEndocrinologymedicine.arteryIsoprenalineInternal medicinecardiovascular systemmedicinebiology.proteinsense organsmedicine.symptomCardiology and Cardiovascular MedicinebusinessVasoconstrictionmedicine.drugJournal of Vascular Research
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Molecular cloning of rat G-protein-coupled receptor kinase 6 (GRK6) from brain tissue, and its mRNA expression in different brain regions and periphe…

1997

The rat G-protein-coupled receptor kinase 6 (GRK6) cDNA was cloned from rat brain tissue by a combination of reverse-transcription polymerase chain reactions (RT-PCR), based on homology to the cloned human GRK6, and rapid amplification of cDNA ends (RACE-PCR). We obtained a clone of 2817 bp with an open reading frame of 1731 bp encoding for a protein of 576 amino acids that is 96.7% identical and 97.9% similar to its human counterpart. mRNA was detectable in all brain areas examined. In addition, GRK6 was expressed in skeletal muscle, small intestine, aorta, liver, heart, lung, thymus, stomach, uterus and kidney.

DNA ComplementaryTranscription GeneticMolecular Sequence DataProtein Serine-Threonine KinasesMolecular cloningBiologyPolymerase Chain ReactionOpen Reading FramesCellular and Molecular NeuroscienceRapid amplification of cDNA endsGTP-Binding ProteinsComplementary DNAGene expressionAnimalsHumansAmino Acid SequenceRNA MessengerCloning MolecularProtein kinase AMolecular BiologyG protein-coupled receptor kinaseMessenger RNABase SequenceSequence Homology Amino AcidBrainReceptor Protein-Tyrosine KinasesG-Protein-Coupled Receptor KinasesMolecular biologyRatsOpen reading frameOrgan SpecificityFemaleSequence AlignmentMolecular Brain Research
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Myocardial G Protein Receptor–Coupled Kinase Expression Correlates With Functional Parameters and Clinical Severity in Advanced Heart Failure

2010

In heart failure (HF), sympathetic hyperactivation induces deleterious effects in myocardial β-adrenergic signaling, with receptor down-regulation and desensitization mediated by G protein receptor-coupled kinases (GRKs). We hypothesised that changes in GRK isoforms may be associated with clinical status in advanced HF, using the Interagency Registry for Mechanically Assisted Circulatory Support (INTERMACS) scale.We included 31 patients with advanced HF undergoing transplantation. According to INTERMACS profiles, mRNA and protein levels of GRK isoforms in left ventricular (LV) myocardium were analyzed and compared with nonfailing LV samples.In failing LV myocardium, GRK2 and GRK5 (but not G…

G-Protein-Coupled Receptor Kinase 5Malemedicine.medical_specialtyG-Protein-Coupled Receptor Kinase 2Down-RegulationPolymerase Chain ReactionSeverity of Illness IndexGene Expression Regulation EnzymologicInternal medicinemedicineHumansRNA MessengerRegistriesReceptorG protein-coupled receptorHeart FailureG protein-coupled receptor kinasebiologybusiness.industryMyocardiumBeta adrenergic receptor kinaseStroke volumeMiddle AgedG-Protein-Coupled Receptor Kinasesmedicine.diseaseTransplantationEndocrinologySpainHeart failureCirculatory systembiology.proteinFemaleHeart-Assist DevicesCardiology and Cardiovascular MedicinebusinessJournal of Cardiac Failure
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β2- and β1-Adrenoceptor Expression Exhibits a Common Regulatory Pattern With GRK2 and GRK5 in Human and Animal Models of Cardiovascular Diseases.

2015

To explore if genic expression of β(1)- or β(2)-adrenoceptors (ARs) exhibits a common regulatory pattern with G protein-coupled receptor kinase (GRK) 2, GRK3, or GRK5 expression, we determined messenger RNA levels for these genes in different tissues from human and animal models of cardiovascular disease. We measured genic expression by qRT polymerase chain reaction in the left and right ventricles or peripheral blood mononuclear cells from healthy (n = 21), hypertensive (n = 20), heart failure (n = 24), and heart transplanted patients (n = 17) or in left ventricle, peripheral blood mononuclear cells, and kidney from spontaneously hypertensive rats or L-N-methyl-arginine-induced hypertensiv…

G-Protein-Coupled Receptor Kinase 5medicine.medical_specialtyG-Protein-Coupled Receptor Kinase 2Heart DiseasesBiologyPeripheral blood mononuclear cellRats Inbred WKYInternal medicineRats Inbred SHRmedicineAnimalsHumansRNA MessengerReceptorGenePharmacologyRegulation of gene expressionMessenger RNAG protein-coupled receptor kinaseKinaseBeta adrenergic receptor kinaseDisease Models AnimalEndocrinologyNG-Nitroarginine Methyl EsterGene Expression RegulationOrgan SpecificityCase-Control StudiesHypertensionbiology.proteinReceptors Adrenergic beta-2Receptors Adrenergic beta-1Cardiology and Cardiovascular MedicineJournal of cardiovascular pharmacology
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Mitochondrial G protein coupled receptor kinase 2 regulates proinflammatory responses in macrophages.

2013

G-protein-coupled receptor kinase 2 (GRK2) levels are elevated in inflammation but its role is not clear yet. Here we show that GRK2 expression is dependent on NFκB transcriptional activity. In macrophages, LPS induces GRK2 accumulation in mitochondria increasing biogenesis. The overexpression of the carboxy-terminal domain of GRK2 (βARK-ct), known to displace GRK2 from plasma membranes, in macrophages induces earlier localization of GRK2 in mitochondria in response to LPS leading to increased mt-DNA transcription, reduced ROS production and cytokines expression. Our study shows the relevance of GRK2 subcellular localization in macrophage’s biology and its potential therapeutic properties i…

LipopolysaccharidesG-Protein-Coupled Receptor Kinase 2BiophysicsβARK-ctGRK2InflammationMitochondrionBiochemistryArticleProinflammatory cytokineMiceStructural BiologyGeneticsmedicineAnimalsHumansReceptorMolecular BiologyInflammationG protein-coupled receptor kinasebiologyKinaseSubcellular localizationBeta adrenergic receptor kinaseMacrophagesCell BiologySubcellular localizationCell biologyMitochondriabiology.proteinmedicine.symptomReactive Oxygen SpeciesSignal Transduction
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The three α1-adrenoceptor subtypes show different spatio-temporal mechanisms of internalization and ERK1/2 phosphorylation

2013

AbstractWe analyzed the kinetic and spatial patterns characterizing activation of the MAP kinases ERK 1 and 2 (ERK1/2) by the three α1-adrenoceptor (α1-AR) subtypes in HEK293 cells and the contribution of two different pathways to ERK1/2 phosphorylation: protein kinase C (PKC)-dependent ERK1/2 activation and internalization-dependent ERK1/2 activation. The different pathways of phenylephrine induced ERK phosphorylation were determined by western blot, using the PKC inhibitor Ro 31-8425, the receptor internalization inhibitor concanavalin A and the siRNA targeting β-arrestin 2. Receptor internalization properties were studied using CypHer5 technology and VSV-G epitope-tagged receptors. Activ…

MAPK/ERK pathwayArrestinsmedia_common.quotation_subjectBlotting WesternKidneyReal-Time Polymerase Chain ReactionImmunoenzyme TechniquesConstitutive activityReceptors Adrenergic alpha-1Concanavalin AHumansRNA MessengerPKCEnzyme InhibitorsPhosphorylationRNA Small InterferingInternalizationProtein kinase AMolecular BiologyCells CulturedProtein Kinase Cbeta-ArrestinsProtein kinase Cmedia_commonMitogen-Activated Protein Kinase 1G protein-coupled receptor kinaseMitogen-Activated Protein Kinase 3ERK1/2biologyReverse Transcriptase Polymerase Chain ReactionKinaseChemistryCell Biologybeta-Arrestin 2Molecular biologyAdrenaline α1 receptorsEndocytosisMitogen-activated protein kinasebiology.proteinPhosphorylationInternalizationSignal TransductionBiochimica et Biophysica Acta (BBA) - Molecular Cell Research
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Rapid cloning of cDNA ends polymerase chain reaction of G-protein-coupled receptor kinase 6: an improved method to determine 5′- and 3′-cDNA ends

1999

Abstract Rapid cloning of 5′- and 3′-cDNA ends polymerase chain reaction (5′-/3′-RACE-PCR) is useful to determine unknown 5′- and 3′-cDNA termini. Even if the method can yield complete cDNA sequences within a couple of days, the RACE procedure bears some characteristic traps and often results in amplification of unspecific PCR-products. Here we used improved 5′- and 3′-RACE-PCR protocols to obtain the complete cDNA sequence of the G-protein-coupled receptor kinase 6 (GRK6) from a rat brain cDNA library. The use of an anchored oligo-(dT) 16 -V-primer in the cDNA synthesis, the addition of single-sided PCR steps prior to the RACE-PCRs and the optimization of the dA-tailing reaction conditions…

MaleDNA ComplementaryNerve Tissue ProteinsProtein Serine-Threonine KinasesBiologylaw.inventionRats Sprague-DawleyRapid amplification of cDNA endslawComplementary DNAAnimalsRNA MessengerCloning MolecularGenePolymerase chain reactionBrain ChemistryCloningMessenger RNAG protein-coupled receptor kinaseReverse Transcriptase Polymerase Chain ReactioncDNA libraryGeneral NeuroscienceReceptor Protein-Tyrosine KinasesG-Protein-Coupled Receptor KinasesMolecular biologyRatsCell biologyBrain Research Protocols
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In human and rat lung membranes [35s]GTPγS binding is a tool for pharmacological characterization of G protein-coupled devucleotide receptors

1999

The P2Y receptor family is activated by extracellular nucleotides such as ATP and UTP. P2Y receptors regulate physiological functions in numerous cell types. In lung, the P2Y2 receptor subtype plays a role in controlling Cl- and fluid transport. Besides ATP or UTP, also diadenosine tetraphosphate (Ap4A), a stable nucleotide, seems to be of physiological importance. In membrane preparations from human and rat lung we applied several diadenosine polyphosphates to investigate whether they act as agonists for G protein-coupled receptors. We assessed this by determining the stimulation of [35S]GTPgammaS binding. Stimulation of [35S]GTPgammaS binding to G proteins has already been successfully ap…

P2Y receptorG proteinGTPgammaSReceptors Cell SurfaceBiologySulfur RadioisotopesGeneral Biochemistry Genetics and Molecular BiologyRadioligand Assaychemistry.chemical_compoundSpecies SpecificityGTP-Binding ProteinsAnimalsHumansGeneral Pharmacology Toxicology and PharmaceuticsReceptorLungG protein-coupled receptorG protein-coupled receptor kinaseMembranesReceptors Purinergic P2General MedicineFluid transportRatschemistryBiochemistryGuanosine 5'-O-(3-Thiotriphosphate)Ap4ALife Sciences
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