Beta-adrenergic receptor kinase 1

Details

Name
Beta-adrenergic receptor kinase 1
Synonyms
  • 2.7.11.15
  • BARK
  • BARK1
  • Beta-ARK-1
  • G-protein coupled receptor kinase 2
  • GRK2
Gene Name
ADRBK1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0010097|Beta-adrenergic receptor kinase 1
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC
SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLVQRGSANGL
Number of residues
689
Molecular Weight
79572.96
Theoretical pI
7.32
GO Classification
Functions
alpha-2A adrenergic receptor binding / ATP binding / beta-adrenergic receptor kinase activity / Edg-2 lysophosphatidic acid receptor binding / G-protein coupled receptor kinase activity / protein kinase activity
Processes
activation of phospholipase C activity / cardiac muscle contraction / desensitization of G-protein coupled receptor protein signaling pathway / epidermal growth factor receptor signaling pathway / fibroblast growth factor receptor signaling pathway / G-protein coupled acetylcholine receptor signaling pathway / heart development / innate immune response / negative regulation of striated muscle contraction / negative regulation of the force of heart contraction by chemical signal / neurotrophin TRK receptor signaling pathway / peptidyl-serine phosphorylation / peptidyl-threonine phosphorylation / positive regulation of catecholamine secretion / receptor internalization / signal transduction / tachykinin receptor signaling pathway / viral entry into host cell / viral genome replication
Components
cytoplasm / cytosol / membrane / plasma membrane / primary cilium
General Function
Protein kinase activity
Specific Function
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner.
Pfam Domain Function
Transmembrane Regions
Not Available
Cellular Location
Cytoplasm
Gene sequence
>lcl|BSEQ0010098|Beta-adrenergic receptor kinase 1 (ADRBK1)
ATGGCGGACCTGGAGGCGGTGCTGGCCGACGTGAGCTACCTGATGGCCATGGAGAAGAGC
AAGGCCACGCCGGCCGCGCGCGCCAGCAAGAAGATCCTGCTGCCCGAGCCCAGCATCCGC
AGTGTCATGCAGAAGTACCTGGAGGACCGGGGCGAGGTGACCTTTGAGAAGATCTTTTCC
CAGAAGCTGGGGTACCTGCTCTTCCGAGACTTCTGCCTGAACCACCTGGAGGAGGCCAGG
CCCTTGGTGGAATTCTATGAGGAGATCAAGAAGTACGAGAAGCTGGAGACGGAGGAGGAG
CGTGTGGCCCGCAGCCGGGAGATCTTCGACTCATACATCATGAAGGAGCTGCTGGCCTGC
TCGCATCCCTTCTCGAAGAGTGCCACTGAGCATGTCCAAGGCCACCTGGGGAAGAAGCAG
GTGCCTCCGGATCTCTTCCAGCCATACATCGAAGAGATTTGTCAAAACCTCCGAGGGGAC
GTGTTCCAGAAATTCATTGAGAGCGATAAGTTCACACGGTTTTGCCAGTGGAAGAATGTG
GAGCTCAACATCCACCTGACCATGAATGACTTCAGCGTGCATCGCATCATTGGGCGCGGG
GGCTTTGGCGAGGTCTATGGGTGCCGGAAGGCTGACACAGGCAAGATGTACGCCATGAAG
TGCCTGGACAAAAAGCGCATCAAGATGAAGCAGGGGGAGACCCTGGCCCTGAACGAGCGC
ATCATGCTCTCGCTCGTCAGCACTGGGGACTGCCCATTCATTGTCTGCATGTCATACGCG
TTCCACACGCCAGACAAGCTCAGCTTCATCCTGGACCTCATGAACGGTGGGGACCTGCAC
TACCACCTCTCCCAGCACGGGGTCTTCTCAGAGGCTGACATGCGCTTCTATGCGGCCGAG
ATCATCCTGGGCCTGGAGCACATGCACAACCGCTTCGTGGTCTACCGGGACCTGAAGCCA
GCCAACATCCTTCTGGACGAGCATGGCCACGTGCGGATCTCGGACCTGGGCCTGGCCTGT
GACTTCTCCAAGAAGAAGCCCCATGCCAGCGTGGGCACCCACGGGTACATGGCTCCGGAG
GTCCTGCAGAAGGGCGTGGCCTACGACAGCAGTGCCGACTGGTTCTCTCTGGGGTGCATG
CTCTTCAAGTTGCTGCGGGGGCACAGCCCCTTCCGGCAGCACAAGACCAAAGACAAGCAT
GAGATCGACCGCATGACGCTGACGATGGCCGTGGAGCTGCCCGACTCCTTCTCCCCTGAA
CTACGCTCCCTGCTGGAGGGGTTGCTGCAGAGGGATGTCAACCGGAGATTGGGCTGCCTG
GGCCGAGGGGCTCAGGAGGTGAAAGAGAGCCCCTTTTTCCGCTCCCTGGACTGGCAGATG
GTCTTCTTGCAGAAGTACCCTCCCCCGCTGATCCCCCCACGAGGGGAGGTGAACGCGGCC
GACGCCTTCGACATTGGCTCCTTCGATGAGGAGGACACAAAAGGAATCAAGTTACTGGAC
AGTGATCAGGAGCTCTACCGCAACTTCCCCCTCACCATCTCGGAGCGGTGGCAGCAGGAG
GTGGCAGAGACTGTCTTCGACACCATCAACGCTGAGACAGACCGGCTGGAGGCTCGCAAG
AAAGCCAAGAACAAGCAGCTGGGCCATGAGGAAGACTACGCCCTGGGCAAGGACTGCATC
ATGCATGGCTACATGTCCAAGATGGGCAACCCCTTCCTGACCCAGTGGCAGCGGCGGTAC
TTCTACCTGTTCCCCAACCGCCTCGAGTGGCGGGGCGAGGGCGAGGCCCCGCAGAGCCTG
CTGACCATGGAGGAGATCCAGTCGGTGGAGGAGACGCAGATCAAGGAGCGCAAGTGCCTG
CTCCTCAAGATCCGCGGTGGGAAACAGTTCATTTTGCAGTGCGATAGCGACCCTGAGCTG
GTGCAGTGGAAGAAGGAGCTGCGCGACGCCTACCGCGAGGCCCAGCAGCTGGTGCAGCGG
GTGCCCAAGATGAAGAACAAGCCGCGCTCGCCCGTGGTGGAGCTGAGCAAGGTGCCGCTG
GTCCAGCGCGGCAGTGCCAACGGCCTCTGA
Chromosome Location
11
Locus
11q13
External Identifiers
ResourceLink
UniProtKB IDP25098
UniProtKB Entry NameARBK1_HUMAN
GenBank Protein ID288308
GenBank Gene IDX61157
GenAtlas IDADRBK1
HGNC IDHGNC:289
General References
  1. Benovic JL, Stone WC, Huebner K, Croce C, Caron MG, Lefkowitz RJ: cDNA cloning and chromosomal localization of the human beta-adrenergic receptor kinase. FEBS Lett. 1991 May 20;283(1):122-6. [Article]
  2. Chuang TT, Sallese M, Ambrosini G, Parruti G, De Blasi A: High expression of beta-adrenergic receptor kinase in human peripheral blood leukocytes. Isoproterenol and platelet activating factor can induce kinase translocation. J Biol Chem. 1992 Apr 5;267(10):6886-92. [Article]
  3. Penn RB, Benovic JL: Structure of the human gene encoding the beta-adrenergic receptor kinase. J Biol Chem. 1994 May 27;269(21):14924-30. [Article]
  4. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  5. Aragay AM, Mellado M, Frade JM, Martin AM, Jimenez-Sainz MC, Martinez-A C, Mayor F Jr: Monocyte chemoattractant protein-1-induced CCR2B receptor desensitization mediated by the G protein-coupled receptor kinase 2. Proc Natl Acad Sci U S A. 1998 Mar 17;95(6):2985-90. [Article]
  6. Oppermann M, Mack M, Proudfoot AE, Olbrich H: Differential effects of CC chemokines on CC chemokine receptor 5 (CCR5) phosphorylation and identification of phosphorylation sites on the CCR5 carboxyl terminus. J Biol Chem. 1999 Mar 26;274(13):8875-85. [Article]
  7. Zahedi RP, Lewandrowski U, Wiesner J, Wortelkamp S, Moebius J, Schutz C, Walter U, Gambaryan S, Sickmann A: Phosphoproteome of resting human platelets. J Proteome Res. 2008 Feb;7(2):526-34. Epub 2007 Dec 19. [Article]
  8. Aziziyeh AI, Li TT, Pape C, Pampillo M, Chidiac P, Possmayer F, Babwah AV, Bhattacharya M: Dual regulation of lysophosphatidic acid (LPA1) receptor signalling by Ral and GRK. Cell Signal. 2009 Jul;21(7):1207-17. doi: 10.1016/j.cellsig.2009.03.011. Epub 2009 Mar 21. [Article]
  9. Burkard TR, Planyavsky M, Kaupe I, Breitwieser FP, Burckstummer T, Bennett KL, Superti-Furga G, Colinge J: Initial characterization of the human central proteome. BMC Syst Biol. 2011 Jan 26;5:17. doi: 10.1186/1752-0509-5-17. [Article]
  10. Fushman D, Najmabadi-Haske T, Cahill S, Zheng J, LeVine H 3rd, Cowburn D: The solution structure and dynamics of the pleckstrin homology domain of G protein-coupled receptor kinase 2 (beta-adrenergic receptor kinase 1). A binding partner of Gbetagamma subunits. J Biol Chem. 1998 Jan 30;273(5):2835-43. [Article]
  11. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, Davies H, Teague J, Butler A, Stevens C, Edkins S, O'Meara S, Vastrik I, Schmidt EE, Avis T, Barthorpe S, Bhamra G, Buck G, Choudhury B, Clements J, Cole J, Dicks E, Forbes S, Gray K, Halliday K, Harrison R, Hills K, Hinton J, Jenkinson A, Jones D, Menzies A, Mironenko T, Perry J, Raine K, Richardson D, Shepherd R, Small A, Tofts C, Varian J, Webb T, West S, Widaa S, Yates A, Cahill DP, Louis DN, Goldstraw P, Nicholson AG, Brasseur F, Looijenga L, Weber BL, Chiew YE, DeFazio A, Greaves MF, Green AR, Campbell P, Birney E, Easton DF, Chenevix-Trench G, Tan MH, Khoo SK, Teh BT, Yuen ST, Leung SY, Wooster R, Futreal PA, Stratton MR: Patterns of somatic mutation in human cancer genomes. Nature. 2007 Mar 8;446(7132):153-8. [Article]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00171ATPinvestigational, nutraceuticalunknownDetails