重組細胞
expressed in baculovirus infected Sf9 cells
產品線
PRECISIO® Kinase
化驗
≥70% (SDS-PAGE)
形狀
buffered aqueous glycerol solution
比活性
4.5-6.1 nmol/min·mg
分子量
~102 kDa
NCBI登錄號
運輸包裝
dry ice
儲存溫度
−70°C
基因資訊
human ... ADRBK1(156)
一般說明
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.
生化／生理作用
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.
外觀
Supplied in 50mM Tris-HCl, pH 7.5, 150mM NaCl, 10mM glutathione, 0.1mM EDTA, 0.25mM DTT, 0.1mM PMSF, 25% glycerol.
準備報告
after opening, aliquot into smaller quantities and store at -70 °C. Avoid repeating handling and multiple freeze/thaw cycles
法律資訊
PRECISIO is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
10 - Combustible liquids
水污染物質分類（WGK）
WGK 1
閃點（°F）
Not applicable
閃點（°C）
Not applicable
分析證明 (COA)
輸入產品批次/批號來搜索 分析證明 (COA)。在產品’s標籤上找到批次和批號，寫有 ‘Lot’或‘Batch’.。
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
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
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)
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)
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