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Mouse Anti-GRK5 ( AA 51-150) Recombinant Antibody (CBFYH-0489) (CBMAB-H1358-FY)


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Summary

Host Animal
Mouse
Specificity
Human
Clone
CBFYH-0489
Antibody Isotype
IgG2a, κ
Application
ELISA

Basic Information

Immunogen
Recombinant protein with GST tag. MW of the GST tag alone is 26 KDa.
Specificity
Human
Antibody Isotype
IgG2a, κ
Clonality
Monoclonal
Application Notes
The COA includes recommended starting dilutions, optimal dilutions should be determined by the end user.

Formulations & Storage [For reference only, actual COA shall prevail!]

Format
Liquid
Storage
Store at +4°C short term (1-2 weeks). Aliquot and store at -20°C long term. Avoid repeated freeze/thaw cycles.
Epitope
AA 51-150

Target

Full Name
G protein-coupled receptor kinase 5
Introduction
This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. It has also been shown to play a role in regulating the motility of polymorphonuclear leukocytes (PMNs).
Entrez Gene ID
2869
UniProt ID
P34947
Alternative Names
G Protein-Coupled Receptor Kinase 5; G Protein-Coupled Receptor Kinase GRK5; EC 2.7.11.16; GPRK5; EC 2.7.11; FP2025
Function
Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein-coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70-interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2-mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G-protein-coupled receptor, LRP6 during Wnt signaling (in vitro).
Biological Process
Adenylate cyclase-modulating G protein-coupled receptor signaling pathway Source: ProtInc
Apoptotic process Source: UniProtKB-KW
G protein-coupled receptor signaling pathway Source: Reactome
Negative regulation of apoptotic process Source: UniProtKB
Positive regulation of cell population proliferation Source: CACAO
Protein autophosphorylation Source: UniProtKB
Protein phosphorylation Source: GO_Central
Regulation of cell cycle Source: CACAO
Regulation of G protein-coupled receptor signaling pathway Source: ProtInc
Regulation of signal transduction Source: GO_Central
Tachykinin receptor signaling pathway Source: BHF-UCL
Wnt signaling pathway Source: UniProtKB-KW
Cellular Location
Cell membrane; Nucleus; Cytoplasm. Predominantly localized at the plasma membrane; targeted to the cell surface through the interaction with phospholipids. Nucleus localization is regulated in a GPCR and Ca2+/calmodulin-dependent fashion.
PTM
Autophosphorylated. Autophosphorylation may play a critical role in the regulation of GRK5 kinase activity.
More Infomation

De Lucia, C., Grisanti, L. A., Borghetti, G., Piedepalumbo, M., Ibetti, J., Lucchese, A. M., ... & Koch, W. J. (2022). G protein-coupled receptor kinase 5 (GRK5) contributes to impaired cardiac function and immune cell recruitment in post-ischemic heart failure. Cardiovascular Research, 118(1), 169-183.

Downes, K., Zhao, X., Gleadall, N. S., McKinney, H., Kempster, C., Batista, J., ... & Ma, P. (2022). G protein–coupled receptor kinase 5 regulates thrombin signaling in platelets via PAR-1. Blood Advances, 6(7), 2319-2330.

Toya, M., Akasaki, Y., Sueishi, T., Kurakazu, I., Kuwahara, M., Uchida, T., ... & Nakashima, Y. (2021). G protein-coupled receptor kinase 5 deletion suppresses synovial inflammation in a murine model of collagen antibody-induced arthritis. Scientific reports, 11(1), 10481.

Guimarães, T. R., Swanson, E., Kofler, J., & Thathiah, A. (2021). G protein‐coupled receptor kinases are associated with Alzheimer's disease pathology. Neuropathology and applied neurobiology, 47(7), 942-957.

Sok, V., Jacinto, A. Z., Peng, N., Eldemerdash, M., Le, L., Tran, P. D., ... & So, C. H. (2021). G protein coupled receptor kinase 5 modifies the nucleolar stress response activated by actinomycin D. Biochemistry and Cell Biology, 99(4), 508-518.

Lagman, J., Sayegh, P., Lee, C. S., Sulon, S. M., Jacinto, A. Z., Sok, V., ... & So, C. H. (2019). G protein-coupled receptor kinase 5 modifies cancer cell resistance to paclitaxel. Molecular and Cellular Biochemistry, 461, 103-118.

Rowlands, R. A., Cato, M. C., Waldschmidt, H. V., Bouley, R. A., Chen, Q., Avramova, L., ... & White, A. D. (2019). Structure-based design of selective, covalent G protein-coupled receptor kinase 5 inhibitors. ACS Medicinal Chemistry Letters, 10(12), 1628-1634.

Yeh, S. T., Zambrano, C. M., Koch, W. J., & Purcell, N. H. (2018). PH domain leucine-rich repeat protein phosphatase 2 (PHLPP2) regulates G-protein–coupled receptor kinase 5 (GRK5)-induced cardiac hypertrophy in vitro. Journal of Biological Chemistry, 293(21), 8056-8064.

Lutz, S. Z., Falcenberg, M., Machicao, F., Peter, A., Kächele, M., Randrianarisoa, E., ... & Kantartzis, K. (2018). Single Nucleotide Polymorphisms in the G-Protein Coupled Receptor Kinase 5 (GRK5) Gene are associated with Plasma LDL-Cholesterol Levels in Humans. Scientific Reports, 8(1), 7745.

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For research use only. Not intended for any clinical use.

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