Grk5

Summary

Gene Symbol: Grk5
Description: G protein-coupled receptor kinase 5
Alias: Gprk5, G protein-coupled receptor kinase 5, g protein-coupled receptor kinase GRK5
Species: mouse
Products:     Grk5

Top Publications

  1. Walker J, Gainetdinov R, Feldman D, McFawn P, Caron M, Lefkowitz R, et al. G protein-coupled receptor kinase 5 regulates airway responses induced by muscarinic receptor activation. Am J Physiol Lung Cell Mol Physiol. 2004;286:L312-9 pubmed
    ..GPCR kinases (GRKs) are important regulators of GPCR desensitization. GRK5, one member of the GRK family, desensitizes central M(2) muscarinic receptors in mice...
  2. Jaber M, Koch W, Rockman H, Smith B, Bond R, Sulik K, et al. Essential role of beta-adrenergic receptor kinase 1 in cardiac development and function. Proc Natl Acad Sci U S A. 1996;93:12974-9 pubmed
  3. Gainetdinov R, Bohn L, Walker J, Laporte S, Macrae A, Caron M, et al. Muscarinic supersensitivity and impaired receptor desensitization in G protein-coupled receptor kinase 5-deficient mice. Neuron. 1999;24:1029-36 pubmed
    G protein-coupled receptor kinase 5 (GRK5) is a member of a family of enzymes that phosphorylate activated G protein-coupled receptors (GPCR)...
  4. Suo Z, Cox A, Bartelli N, Rasul I, Festoff B, Premont R, et al. GRK5 deficiency leads to early Alzheimer-like pathology and working memory impairment. Neurobiol Aging. 2007;28:1873-88 pubmed
    G-protein coupled receptor kinase-5 (GRK5) deficiency has been linked to early Alzheimer's disease in humans and mouse models of the disease...
  5. Wang F, Wang L, Shen M, Ma L. GRK5 deficiency decreases diet-induced obesity and adipogenesis. Biochem Biophys Res Commun. 2012;421:312-7 pubmed publisher
    ..In this study, we found that G protein coupled receptor (GPCR) kinase 5 (GRK5) was expressed at a relatively high level in the white adipose tissue...
  6. Packiriswamy N, Parvataneni S, Parameswaran N. Overlapping and distinct roles of GRK5 in TLR2-, and TLR3-induced inflammatory response in vivo. Cell Immunol. 2012;272:107-11 pubmed publisher
    G-protein coupled receptor kinase-5 (GRK5) is a recently described NF?B regulator in TLR4 signaling pathway...
  7. Patial S, Shahi S, Saini Y, Lee T, Packiriswamy N, Appledorn D, et al. G-protein coupled receptor kinase 5 mediates lipopolysaccharide-induced NF?B activation in primary macrophages and modulates inflammation in vivo in mice. J Cell Physiol. 2011;226:1323-33 pubmed publisher
    G-protein coupled receptor kinase-5 (GRK5) is a serine/threonine kinase discovered for its role in the regulation of G-protein coupled receptor signaling...
  8. Chen X, Zhu H, Yuan M, Fu J, Zhou Y, Ma L. G-protein-coupled receptor kinase 5 phosphorylates p53 and inhibits DNA damage-induced apoptosis. J Biol Chem. 2010;285:12823-30 pubmed publisher
    ..Knockdown GRK5 in osteosarcoma cells inhibits DNA damage-induced apoptosis via a p53-mediated mechanism...
  9. Nanjidsuren T, Park C, Sim B, Kim S, Chang K, Kang M, et al. GRK5-Knockout Mice Generated by TALEN-Mediated Gene Targeting. Anim Biotechnol. 2016;27:223-30 pubmed publisher
    ..TALEN vectors were designed to target exons 1, 3, and 5 of the mouse GRK5 gene. Flow cytometry showed that the activity of the TALEN mRNAs targeted to exons 1, 3, and 5 was 8.7%, 9...

More Information

Publications38

  1. He M, Singh P, Cheng S, Zhang Q, Peng W, Ding X, et al. GRK5 Deficiency Leads to Selective Basal Forebrain Cholinergic Neuronal Vulnerability. Sci Rep. 2016;6:26116 pubmed publisher
    ..over-express the Swedish mutant human β-amyloid precursor protein gene with G protein-coupled receptor kinase-5 (GRK5) knockout mice...
  2. Packiriswamy N, Steury M, McCabe I, Fitzgerald S, Parameswaran N. Bacterial Dose-Dependent Role of G Protein-Coupled Receptor Kinase 5 in Escherichia coli-Induced Pneumonia. Infect Immun. 2016;84:1633-1641 pubmed publisher
    G protein-coupled receptor kinase 5 (GRK5) is a serine/threonine kinase previously shown to mediate polymicrobial sepsis-induced inflammation...
  3. Hullmann J, Grisanti L, Makarewich C, Gao E, Gold J, Chuprun J, et al. GRK5-mediated exacerbation of pathological cardiac hypertrophy involves facilitation of nuclear NFAT activity. Circ Res. 2014;115:976-85 pubmed publisher
    ..Both GRK2 and GRK5, the predominant GRKs expressed in the heart, have been shown to be upregulated in failing human myocardium...
  4. Chen Y, Wang F, Long H, Chen Y, Wu Z, Ma L. GRK5 promotes F-actin bundling and targets bundles to membrane structures to control neuronal morphogenesis. J Cell Biol. 2011;194:905-20 pubmed publisher
    Neuronal morphogenesis requires extensive membrane remodeling and cytoskeleton dynamics. In this paper, we show that GRK5, a G protein-coupled receptor kinase, is critically involved in neurite outgrowth, dendrite branching, and spine ..
  5. Li L, Rasul I, Liu J, Zhao B, Tang R, Premont R, et al. Augmented axonal defects and synaptic degenerative changes in female GRK5 deficient mice. Brain Res Bull. 2009;78:145-51 pubmed publisher
    Recent studies suggested that G protein-coupled receptor kinase 5 (GRK5) deficiency plays a significant role in early Alzheimer's disease (AD) pathogenesis, and that the GRK5 knockout (GRK5KO) mouse displays an early Alzheimer-like ..
  6. Wu J, Goswami R, Cai X, Exum S, Huang X, Zhang L, et al. Regulation of the platelet-derived growth factor receptor-beta by G protein-coupled receptor kinase-5 in vascular smooth muscle cells involves the phosphatase Shp2. J Biol Chem. 2006;281:37758-72 pubmed
    ..In mouse aortic SMCs, however, we found that prolonged PDGFRbeta activation engendered down-regulation of GRK5, but not GRK2; moreover, GRK5 and PDGFRbeta were coordinately up-regulated in SMCs from atherosclerotic arteries...
  7. Cho M, Rao M, Koch W, Thomas S, Palmiter R, Rockman H. Enhanced contractility and decreased beta-adrenergic receptor kinase-1 in mice lacking endogenous norepinephrine and epinephrine. Circulation. 1999;99:2702-7 pubmed
    ..This animal model will be valuable in testing whether NE is required for the pathogenesis of heart failure through mating strategies that cross the dbh-/- mouse into genetically engineered models of heart failure. ..
  8. Premont R, Macrae A, Aparicio S, Kendall H, Welch J, Lefkowitz R. The GRK4 subfamily of G protein-coupled receptor kinases. Alternative splicing, gene organization, and sequence conservation. J Biol Chem. 1999;274:29381-9 pubmed
    ..Comparison of the amino acid sequences of GRKs from various mammalian species indicates that GRK2, GRK5, and GRK6 exhibit a remarkably high degree of sequence conservation, whereas GRK1 and particularly GRK4 have ..
  9. Fong A, Premont R, Richardson R, Yu Y, Lefkowitz R, Patel D. Defective lymphocyte chemotaxis in beta-arrestin2- and GRK6-deficient mice. Proc Natl Acad Sci U S A. 2002;99:7478-83 pubmed
    ..Knockouts of beta-arrestin2, GRK5, and GRK6 were examined because all three proteins are expressed at high levels in purified mouse CD3+ T and B220+ ..
  10. Islam K, Bae J, Gao E, Koch W. Regulation of nuclear factor ?B (NF-?B) in the nucleus of cardiomyocytes by G protein-coupled receptor kinase 5 (GRK5). J Biol Chem. 2013;288:35683-9 pubmed publisher
    G protein-coupled receptor kinase 5 GRK5 plays a key role in regulating cardiac signaling and its expression is increased in heart failure...
  11. Rajagopal K, Whalen E, Violin J, Stiber J, Rosenberg P, Premont R, et al. Beta-arrestin2-mediated inotropic effects of the angiotensin II type 1A receptor in isolated cardiac myocytes. Proc Natl Acad Sci U S A. 2006;103:16284-9 pubmed
    ..knockout mice (GRK2(+/-)) exhibited augmented responses to SII in comparison to ANG, whereas those from GRK5 KO mice did not differ from those from WT mice...
  12. Tarrant T, Rampersad R, Esserman D, Rothlein L, Liu P, Premont R, et al. Granulocyte chemotaxis and disease expression are differentially regulated by GRK subtype in an acute inflammatory arthritis model (K/BxN). Clin Immunol. 2008;129:115-22 pubmed publisher
    ..Clinical, histologic, and cytokine responses in GRK6-/-, GRK5-/-, GRK2+/-, and wildtype mice were evaluated using K/BxN serum transfer...
  13. Li L, Liu J, Suo W. GRK5 deficiency exaggerates inflammatory changes in TgAPPsw mice. J Neuroinflammation. 2008;5:24 pubmed publisher
    Deficiency of membrane G-protein coupled receptor (GPCR) kinase-5 (GRK5) recently has been linked to early AD pathogenesis, and has been suggested to contribute to augmented microglial activation in vitro by sensitizing relevant GPCRs...
  14. Patial S, Luo J, Porter K, Benovic J, Parameswaran N. G-protein-coupled-receptor kinases mediate TNF?-induced NF?B signalling via direct interaction with and phosphorylation of I?B?. Biochem J. 2009;425:169-78 pubmed publisher
    ..Furthermore, we also find that GRK5 but not GRK2 phosphorylates I?B? at the same amino acid residues (Ser32/36) as that of IKK?...
  15. Loniewski K, Shi Y, Pestka J, Parameswaran N. Toll-like receptors differentially regulate GPCR kinases and arrestins in primary macrophages. Mol Immunol. 2008;45:2312-22 pubmed publisher
    ..Compared to this, activation of TLR2, 4, and 7 (but not TLR3) significantly decrease GRK5 and 6 protein levels. Surprisingly, GRK2 protein levels are markedly increased by TLR2, 3, 4 and 7...
  16. Singh P, Peng W, Zhang Q, Ding X, Suo W. GRK5 deficiency leads to susceptibility to intermittent hypoxia-induced cognitive impairment. Behav Brain Res. 2016;302:29-34 pubmed publisher
    ..G protein-coupled receptor kinase-5 (GRK5) deficiency is recently found to render subjects more susceptible to cognitive impairment triggered by over-..
  17. Glück L, Loktev A, Mouledous L, Mollereau C, Law P, Schulz S. Loss of morphine reward and dependence in mice lacking G protein-coupled receptor kinase 5. Biol Psychiatry. 2014;76:767-74 pubmed publisher
    ..place preference test, we investigated opioid-related antinociception and reward effects in mice lacking GRK3 or GRK5. Etonitazene and fentanyl stimulated the in vivo phosphorylation of multiple carboxyl-terminal phosphate acceptor ..
  18. Packiriswamy N, Lee T, Raghavendra P, Durairaj H, Wang H, Parameswaran N. G-protein-coupled receptor kinase-5 mediates inflammation but does not regulate cellular infiltration or bacterial load in a polymicrobial sepsis model in mice. J Innate Immun. 2013;5:401-13 pubmed publisher
    ..G-protein-coupled receptor kinase-5 (GRK5) is an evolutionarily conserved regulator of the NF?B pathway...
  19. Wang L, Shen M, Wang F, Ma L. GRK5 ablation contributes to insulin resistance. Biochem Biophys Res Commun. 2012;429:99-104 pubmed publisher
    The G-protein-coupled receptor kinase 5 (GRK5) is an important member of the threonine/serine kinase family that phosphorylates and regulates the G-protein-coupled receptor (GPCR) signaling pathway...
  20. Gold J, Gao E, Shang X, Premont R, Koch W. Determining the absolute requirement of G protein-coupled receptor kinase 5 for pathological cardiac hypertrophy: short communication. Circ Res. 2012;111:1048-53 pubmed
    ..Cardiac-specific overexpression of G proteinen-coupled receptor kinase-5 (GRK5) has previously been shown to possess nuclear activity as a HDAC5 kinase, promoting an intolerance to in vivo ..
  21. Noma T, Lemaire A, Naga Prasad S, Barki Harrington L, Tilley D, Chen J, et al. Beta-arrestin-mediated beta1-adrenergic receptor transactivation of the EGFR confers cardioprotection. J Clin Invest. 2007;117:2445-58 pubmed
  22. Cheng S, Li L, He S, Liu J, Sun Y, He M, et al. GRK5 deficiency accelerates {beta}-amyloid accumulation in Tg2576 mice via impaired cholinergic activity. J Biol Chem. 2010;285:41541-8 pubmed publisher
    Membrane G protein-coupled receptor kinase 5 (GRK5) deficiency is linked to Alzheimer disease, yet its precise roles in the disease pathogenesis remain to be delineated...
  23. Nakaya M, Chikura S, Watari K, Mizuno N, Mochinaga K, Mangmool S, et al. Induction of cardiac fibrosis by ?-blocker in G protein-independent and G protein-coupled receptor kinase 5/?-arrestin2-dependent Signaling pathways. J Biol Chem. 2012;287:35669-77 pubmed publisher
    ..1)-adrenergic receptor and ?-arrestin2 by metoprolol was impaired in the G protein-coupled receptor kinase 5 (GRK5)-knockdown cells. Metoprolol-induced cardiac fibrosis led to cardiac dysfunction...
  24. Liu J, Rasul I, Sun Y, Wu G, Li L, Premont R, et al. GRK5 deficiency leads to reduced hippocampal acetylcholine level via impaired presynaptic M2/M4 autoreceptor desensitization. J Biol Chem. 2009;284:19564-71 pubmed publisher
    G protein-coupled receptor kinase 5 (GRK5) deficiency has been linked recently to early Alzheimer disease (AD), but the mechanism by which GRK5 deficiency may contribute to AD pathogenesis remains elusive...
  25. Rakesh K, Yoo B, Kim I, Salazar N, Kim K, Rockman H. beta-Arrestin-biased agonism of the angiotensin receptor induced by mechanical stress. Sci Signal. 2010;3:ra46 pubmed publisher
    ..These data show that the heart responds to acute increases in mechanical stress by activating beta-arrestin-mediated cell survival signals. ..
  26. Martini J, Raake P, Vinge L, DeGeorge B, DeGeorge B, Chuprun J, et al. Uncovering G protein-coupled receptor kinase-5 as a histone deacetylase kinase in the nucleus of cardiomyocytes. Proc Natl Acad Sci U S A. 2008;105:12457-62 pubmed publisher
    ..In cardiomyocytes, GRK2 and GRK5 are two GRKs important for myocardial regulation, and both have been shown to be up-regulated in the dysfunctional ..
  27. Chen M, Philipp M, Wang J, Premont R, Garrison T, Caron M, et al. G Protein-coupled receptor kinases phosphorylate LRP6 in the Wnt pathway. J Biol Chem. 2009;284:35040-8 pubmed publisher
    ..We found that G protein-coupled receptor kinases 5 and 6 (GRK5/6), traditionally known to phosphorylate and desensitize 7TM G protein-coupled receptors, directly phosphorylate ..
  28. Wu J, Zhang L, Fanaroff A, Cai X, Sharma K, Brian L, et al. G protein-coupled receptor kinase-5 attenuates atherosclerosis by regulating receptor tyrosine kinases and 7-transmembrane receptors. Arterioscler Thromb Vasc Biol. 2012;32:308-16 pubmed publisher
    G protein-coupled receptor kinase-5 (GRK5) is a widely expressed Ser/Thr kinase that regulates several atherogenic receptors and may activate or inhibit nuclear factor-?B (NF-?B)...
  29. Keys J, Zhou R, Harris D, Druckman C, Eckhart A. Vascular smooth muscle overexpression of G protein-coupled receptor kinase 5 elevates blood pressure, which segregates with sex and is dependent on Gi-mediated signaling. Circulation. 2005;112:1145-53 pubmed
    ..We generated transgenic mice with approximately 2-fold vascular smooth muscle (VSM)-specific overexpression of GRK5 to recapitulate a selective aspect of hypertension and understand the impact on GPCR regulation of BP...