mProX™ Human GRK4 Stable Cell Line

Sub Cat	Product Name	Target Protein Species	Host Cell Type	Assay Types	Inquiry	Datasheet
S01YF-1122-KX1154	Magic™ Human GPRK4(GRK4) in Vitro Assay	Human		Kinase Assay

Product Information

Target Protein

GRK4

Target Family

Kinases/Enzyme Drug Discovery Assays and Products

Target Protein Species

Human

Host Cell Type

CHO-K1; HEK293

Target Classification

Kinase Cell Lines

Target Research Area

Cardiovascular Research

Related Diseases

Hypertension, Essential and Hermansky-Pudlak Syndrome 3. Among its related pathways are Visual phototransduction and Myometrial relaxation and contraction pathways

Gene ID

2868

UniProt ID

P32298

Product Properties

Biosafety Level

Level 1

Activity

Yes

Quantity

10⁶ cells per vial

Applications

Encoded by the GRK4 gene in humans is the enzyme known as G protein-coupled receptor kinase 4 (GRK4). The G protein-coupled receptor kinase subfamily of the Ser/Thr protein kinase family, which this gene encodes, is primarily related to GRK5 and GRK6. In order to facilitate the binding of an arrestin protein to the receptor, G protein-coupled receptor kinases phosphorylate active G protein-coupled receptors. When an arrestin binds to an active, phosphorylated receptor, heterotrimeric G protein transducer proteins are not stimulated by the receptor, which inhibits cellular communication and causes receptor desensitization. Additionally Receptor signaling via arrestin partner proteins is also made possible by arrestin binding to an active, phosphorylated receptor. Thus, G protein-coupled receptors use the GRK/arrestin system as a signaling switch. The customized GRK4 stable cell line can be used in antibody discovery and development, potential drug candidate screening and signaling pathway researches.

Protocols

Please visit our protocols page.

Customer Reviews

chat Richard

The results have been consistent and reliable, providing crucial insights into GRK4 research. Dec 02 2022

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chat Timothy

The GRK4 cell line has streamlined my assays and allowed me to obtain accurate data. Oct 26 2021

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FAQ

Any questions about our products? Please visit our frequently asked questions page.

Published Data

Fig.1 Change of protein levels during GRK4-induced senescence in HEK 293 cells.

Following transfection with pEGFP-GRK4 plasmids, GRK4(+) and GRK4(-) cells were sorted by flow cytometry. GRK4 overexpression's effects on p53 and p21 levels. MCF-7 cells treated with ADM were used as the antibody control.

Ref: Xiao, Pingping, et al. "G protein-coupled receptor kinase 4-induced cellular senescence and its senescence-associated gene expression profiling." Experimental cell research 360.2 (2017): 273-280.

Pubmed: 28912086

DOI: 10.1016/j.yexcr.2017.09.017

Research Highlights

Variants of GRK4 have been connected to reduced Na excretion, hypertension in humans and animal models, and the therapeutic response to dietary Na restriction and antihypertensive medication. It might also explain the variations in hypertension observed among various demographic groups coming from different geographical regions and serve as a foundation for pharmacogenomic approaches to hypertension management.
Rayner, Brian, and Raj Ramesar. "The importance of G protein-coupled receptor kinase 4 (GRK4) in pathogenesis of salt sensitivity, salt sensitive hypertension and response to antihypertensive treatment." International Journal of Molecular Sciences 16.3 (2015): 5741-5749.
Pubmed: 25775155 DOI: 10.3390/ijms16035741

Arrestin binding to phosphorylated GPCRs that are inactive implies that G protein-independent signaling is regulated by the complement of GRKs in the cell as well as agonist activity.
Li, Lingyong, et al. "G protein-coupled receptor kinases of the GRK4 protein subfamily phosphorylate inactive G protein-coupled receptors (GPCRs)." Journal of Biological Chemistry 290.17 (2015): 10775-10790.
Pubmed: 25770216 DOI: 10.1074/jbc.M115.644773