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Gene Review

Adrbk1  -  adrenergic, beta, receptor kinase 1

Rattus norvegicus

Synonyms: BARK1, Beta-ARK-1, Beta-adrenergic receptor kinase 1, G-protein-coupled receptor kinase 2, GRK-2, ...
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Disease relevance of Adrbk1


High impact information on Adrbk1


Chemical compound and disease context of Adrbk1


Biological context of Adrbk1


Anatomical context of Adrbk1

  • Immunohistochemical analysis of myocardial tissue sections and Western blot analysis of isolated cells revealed localization of GRK2 and beta-arrestin-1 predominantly in endothelial cells [1].
  • In addition, we analyzed GRK2 expression in the hippocampus by immunohistochemistry [2].
  • The reported changes in GRK2 levels and in the receptor/kinase ratio predict alterations in adrenergic receptor desensitization and signal transduction efficacy consistent with those observed in thyroid disorders, thus suggesting a relevant role for the modulation of GRK2 expression in this physiopathological condition [3].
  • We questioned the effect of age on caveolin-1 expression and interaction between caveolin-1 and GRK-2 in vascular smooth muscle (VSM) isolated from 2-, 6-, 12-, and 24-mo-old male Fischer 344 rat aorta [16].
  • Myocyte redistribution of GRK2 and GRK5 in hypertensive, heart-failure-prone rats [4].

Associations of Adrbk1 with chemical compounds


Co-localisations of Adrbk1


Regulatory relationships of Adrbk1

  • Similarly, depletion of GRK-2 protein by stable transfection of full-length antisense OK-GRK2 cDNA blocked the desensitization of alpha2C-adrenergic receptors but not of 5-HT1B receptors [20].

Other interactions of Adrbk1

  • In conclusion, myocardial mRNA and protein levels of GRK2, GRK5, and beta-arrestin-1 are induced in postinfarction failure in rats [1].
  • Coexpression of GRK2 and beta-arrestin-2 suppressed GnRH-induced IP3 production more than that of either alone [21].
  • We also found that the mRNA ratio of B2AR and BARK1 was well correlated with the preservation of the LVPDP [22].
  • Adeno-GRK2-infected cells showed a GRK2 immunoreactivity of about 2.5 (OD405) and LH secretion of 2.5 ng/ml [13].
  • GRK2 is a member of the G protein-coupled receptor kinase family that phosphorylates the activated form of beta-adrenergic and other G protein-coupled receptors and plays an important role in their desensitization and modulation [3].

Analytical, diagnostic and therapeutic context of Adrbk1


  1. Myocardial distribution and regulation of GRK and beta-arrestin isoforms in congestive heart failure in rats. Vinge, L.E., Øie, E., Andersson, Y., Grøgaard, H.K., Andersen, G., Attramadal, H. Am. J. Physiol. Heart Circ. Physiol. (2001) [Pubmed]
  2. Hypoxia/ischemia modulates G protein-coupled receptor kinase 2 and beta-arrestin-1 levels in the neonatal rat brain. Lombardi, M.S., van den Tweel, E., Kavelaars, A., Groenendaal, F., van Bel, F., Heijnen, C.J. Stroke (2004) [Pubmed]
  3. Effect of hypothyroidism on G protein-coupled receptor kinase 2 expression levels in rat liver, lung, and heart. Penela, P., Barradas, M., Alvarez-Dolado, M., Muñoz, A., Mayor, F. Endocrinology (2001) [Pubmed]
  4. Myocyte redistribution of GRK2 and GRK5 in hypertensive, heart-failure-prone rats. Yi, X.P., Gerdes, A.M., Li, F. Hypertension (2002) [Pubmed]
  5. A crucial role for GRK2 in regulation of endothelial cell nitric oxide synthase function in portal hypertension. Liu, S., Premont, R.T., Kontos, C.D., Zhu, S., Rockey, D.C. Nat. Med. (2005) [Pubmed]
  6. Beta-adrenergic receptor kinase-2 and beta-arrestin-2 as mediators of odorant-induced desensitization. Dawson, T.M., Arriza, J.L., Jaworsky, D.E., Borisy, F.F., Attramadal, H., Lefkowitz, R.J., Ronnett, G.V. Science (1993) [Pubmed]
  7. Albuterol-induced downregulation of Gsalpha accounts for pulmonary beta(2)-adrenoceptor desensitization in vivo. Finney, P.A., Belvisi, M.G., Donnelly, L.E., Chuang, T.T., Mak, J.C., Scorer, C., Barnes, P.J., Adcock, I.M., Giembycz, M.A. J. Clin. Invest. (2000) [Pubmed]
  8. A beta-adrenergic receptor kinase-like enzyme is involved in olfactory signal termination. Schleicher, S., Boekhoff, I., Arriza, J., Lefkowitz, R.J., Breer, H. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
  9. Phosphatidylinositol 3-kinase offsets cAMP-mediated positive inotropic effect via inhibiting Ca2+ influx in cardiomyocytes. Leblais, V., Jo, S.H., Chakir, K., Maltsev, V., Zheng, M., Crow, M.T., Wang, W., Lakatta, E.G., Xiao, R.P. Circ. Res. (2004) [Pubmed]
  10. Cell type-specific angiotensin II-evoked signal transduction pathways: critical roles of Gbetagamma subunit, Src family, and Ras in cardiac fibroblasts. Zou, Y., Komuro, I., Yamazaki, T., Kudoh, S., Aikawa, R., Zhu, W., Shiojima, I., Hiroi, Y., Tobe, K., Kadowaki, T., Yazaki, Y. Circ. Res. (1998) [Pubmed]
  11. Role of mitogen-activated protein kinase pathway in prostaglandin F2alpha-induced rat puerperal uterine contraction. Ohmichi, M., Koike, K., Kimura, A., Masuhara, K., Ikegami, H., Ikebuchi, Y., Kanzaki, T., Touhara, K., Sakaue, M., Kobayashi, Y., Akabane, M., Miyake, A., Murata, Y. Endocrinology (1997) [Pubmed]
  12. Rapid agonist-induced beta-adrenergic receptor kinase translocation in C6 glioma cells. García-Higuera, I., Mayor, F. FEBS Lett. (1992) [Pubmed]
  13. High efficiency method for gene transfer in normal pituitary gonadotropes: adenoviral-mediated expression of G protein-coupled receptor kinase 2 suppresses luteinizing hormone secretion. Neill, J.D., Musgrove, L.C., Duck, L.W., Sellers, J.C. Endocrinology (1999) [Pubmed]
  14. Vascular dysfunction in human and rat cirrhosis: role of receptor-desensitizing and calcium-sensitizing proteins. Hennenberg, M., Trebicka, J., Biecker, E., Schepke, M., Sauerbruch, T., Heller, J. Hepatology (2007) [Pubmed]
  15. Angiotensin receptor blockade improves myocardial beta-adrenergic receptor signaling in postinfarction left ventricular remodeling: a possible link between beta-adrenergic receptor kinase-1 and protein kinase C epsilon isoform. Takahashi, T., Anzai, T., Yoshikawa, T., Maekawa, Y., Mahara, K., Iwata, M., Hammond, H.K., Ogawa, S. J. Am. Coll. Cardiol. (2004) [Pubmed]
  16. Decline in caveolin-1 expression and scaffolding of G protein receptor kinase-2 with age in Fischer 344 aortic vascular smooth muscle. Schutzer, W.E., Reed, J.F., Mader, S.L. Am. J. Physiol. Heart Circ. Physiol. (2005) [Pubmed]
  17. Roles of phosphorylation-dependent and -independent mechanisms in the regulation of M1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons. Willets, J.M., Nahorski, S.R., Challiss, R.A. J. Biol. Chem. (2005) [Pubmed]
  18. Beta-adrenergic receptor trafficking by exercise in rat adipocytes: roles of G-protein-coupled receptor kinase-2, beta-arrestin-2, and the ubiquitin-proteasome pathway. Ogasawara, J., Sanpei, M., Rahman, N., Sakurai, T., Kizaki, T., Hitomi, Y., Ohno, H., Izawa, T. FASEB J. (2006) [Pubmed]
  19. Role of cytoplasmic tail of the type 1A angiotensin II receptor in agonist- and phorbol ester-induced desensitization. Tang, H., Guo, D.F., Porter, J.P., Wanaka, Y., Inagami, T. Circ. Res. (1998) [Pubmed]
  20. Receptor selectivity of the cloned opossum G protein-coupled receptor kinase 2 (GRK2) in intact opossum kidney cells: role in desensitization of endogenous alpha2C-adrenergic but not serotonin 1B receptors. Lembo, P.M., Ghahremani, M.H., Albert, P.R. Mol. Endocrinol. (1999) [Pubmed]
  21. Potential regulatory roles for G protein-coupled receptor kinases and beta-arrestins in gonadotropin-releasing hormone receptor signaling. Neill, J.D., Duck, L.W., Musgrove, L.C., Sellers, J.C. Endocrinology (1998) [Pubmed]
  22. Activation of beta2-adrenergic receptor plays a pivotal role in generating the protective effect of ischemic preconditioning in rat hearts. Mieno, S., Horimoto, H., Sawa, Y., Watanabe, F., Furuya, E., Horimoto, S., Kishida, K., Sasaki, S. Scand. Cardiovasc. J. (2005) [Pubmed]
  23. S100A1 gene therapy preserves in vivo cardiac function after myocardial infarction. Pleger, S.T., Remppis, A., Heidt, B., Völkers, M., Chuprun, J.K., Kuhn, M., Zhou, R.H., Gao, E., Szabo, G., Weichenhan, D., Müller, O.J., Eckhart, A.D., Katus, H.A., Koch, W.J., Most, P. Mol. Ther. (2005) [Pubmed]
  24. Endogenous G protein-coupled receptor kinase 6 triggers homologous beta-adrenergic receptor desensitization in primary uterine smooth muscle cells. Simon, V., Robin, M.T., Legrand, C., Cohen-Tannoudji, J. Endocrinology (2003) [Pubmed]
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