SRP5034

Sigma-Aldrich

GRK2、活性型、GSTタグ融合 ヒト

PRECISIO® Kinase, recombinant, expressed in baculovirus infected Sf9 cells, ≥70% (SDS-PAGE), buffered aqueous glycerol solution

別名:
BARK1, ADRBK1, FLJ16718, β-ARK1

リコンビナント

expressed in baculovirus infected Sf9 cells

製品ライン

PRECISIO® Kinase

アッセイ

≥70% (SDS-PAGE)

形態

buffered aqueous glycerol solution

specific activity

4.5-6.1 nmol/min·mg

分子量

~102 kDa

NCBIアクセッション番号

出荷済み

dry ice

保管温度

−70°C

Gene Information

human ... ADRBK1(156)

詳細

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.

生物化学的/生理学的作用

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.

物理的形状

50 mM Tris-HCl(pH 7.5, 150 mM NaCl, 10 mMグルタチオン, 0.1 mM EDTA, 0.25 mM DTT, 0.1 mM PMSF, 25%グリセロール含有)を用いた溶液として調製されています。

調製ノート

開封後はそれぞれの目的に応じて少量ずつ分注し、-70°Cで保存してください。また、取扱いや凍結融解について、繰り返しのご使用は避けてください。

法的情報

PRECISIO is a registered trademark of Sigma-Aldrich Co. LLC

RIDADR

NONH for all modes of transport

ドイツ水質汚染分類

WGK 1

引火点(°F)

Not applicable

引火点(℃)

Not applicable

試験成績書(COA)
原産地証明書(COO)
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 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)
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 kinase 2 (GRK2) inhibitors: current trends and future perspectives
Guccione M, et al.
Journal of Medicinal Chemistry, 59(20), 9277-9294 (2016)

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