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Kluczowe dokumenty
SRP5034
GRK2, active, GST tagged human
PRECISIO® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution
Synonim(y):
β-ARK1, ADRBK1, BARK1, FLJ16718
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About This Item
Kod UNSPSC:
12352200
NACRES:
NA.77
rekombinowane
expressed in baculovirus infected Sf9 cells
linia produktu
PRECISIO® Kinase
Próba
≥70% (SDS-PAGE)
Postać
buffered aqueous glycerol solution
aktywność właściwa
4.5-6.1 nmol/min·mg
masa cząsteczkowa
~102 kDa
numer dostępu NCBI
Warunki transportu
dry ice
temp. przechowywania
−70°C
informacje o genach
human ... ADRBK1(156)
Opis ogólny
G-protein-coupled receptor kinase 2 (GRK2), which is officially known as adrenergic, beta, receptor kinase 1 (ADRBK1), gene codes for a 689 amino acid protein, that is of 79.573kDa. This gene has 12 catalytic region subdomains. GRK2 is expressed in the vascular endothelium, arterial smooth muscle, myocardium, kidney and in the renal proximal tubule. It is mapped to human chromosome 11q13.
Działania biochem./fizjol.
G-protein-coupled receptor kinase 2 (GRK2) or ADRBK1 is a ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G protein-coupled receptors. GRK2 phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart. RAF kinase inhibitor protein RKIP is a physiologic inhibitor of GRK2. After stimulation of G protein-coupled receptors, RKIP dissociates from its known target, RAF1 to associate with GRK2 and block its activity. G-protein-coupled receptor kinase 2 (GRK2) controls several intracellular mechanisms. It helps to maintain the structure and activities of the heart. Hence it participates in several cardiovascular diseases. GRK2 also modulates ion and fluid transport and eventually, blood pressure. It increases the synthesis of mitochondrial superoxide and reduces oxygen utilization and ATP synthesis. This protein serves as a major onco-modulator.
Postać fizyczna
Supplied in 50mM Tris-HCl, pH 7.5, 150mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25mM DTT, 0.1mM PMSF, 25% glycerol.
Uwaga dotycząca przygotowania
after opening, aliquot into smaller quantities and store at -70 °C. Avoid repeating handling and multiple freeze/thaw cycles
Informacje prawne
PRECISIO is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania
10 - Combustible liquids
Klasa zagrożenia wodnego (WGK)
WGK 1
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
Certyfikaty analizy (CoA)
Poszukaj Certyfikaty analizy (CoA), wpisując numer partii/serii produktów. Numery serii i partii można znaleźć na etykiecie produktu po słowach „seria” lub „partia”.
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Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.
H A Rockman et al.
Proceedings of the National Academy of Sciences of the United States of America, 95(12), 7000-7005 (1998-06-17)
Heart failure is accompanied by severely impaired beta-adrenergic receptor (betaAR) function, which includes loss of betaAR density and functional uncoupling of remaining receptors. An important mechanism for the rapid desensitization of betaAR function is agonist-stimulated receptor phosphorylation by the betaAR
G protein-coupled receptor kinases: Crucial regulators of blood pressure
Yang J, et al.
Journal of the American Heart Association, 5(7), e003519-e003519 (2016)
G protein-coupled receptor kinase 2 (GRK2) promotes breast tumorigenesis through a HDAC6-Pin1 axis
Nogues LR, et al.
EBioMedicine, 13, 132-145 (2016)
G-protein-coupled receptor kinase 2 (GRK2) inhibitors: current trends and future perspectives
Guccione M, et al.
Journal of Medicinal Chemistry, 59(20), 9277-9294 (2016)
Kristina Lorenz et al.
Nature, 426(6966), 574-579 (2003-12-05)
Feedback inhibition is a fundamental principle in signal transduction allowing rapid adaptation to different stimuli. In mammalian cells, the major feedback inhibitor for G-protein-coupled receptors (GPCR) is G-protein-coupled receptor kinase 2 (GRK-2), which phosphorylates activated receptors, uncouples them from G
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