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Aliases for GRK2 Gene

Aliases for GRK2 Gene

  • G Protein-Coupled Receptor Kinase 2 2 3 5
  • EC 2.7.11.15 4 61
  • Beta-ARK-1 3 4
  • ADRBK1 3 4
  • BARK1 3 4
  • Adrenergic, Beta, Receptor Kinase 1 2
  • G-Protein Coupled Receptor Kinase 2 4
  • Adrenergic Beta Receptor Kinase 1 3
  • Beta-Adrenergic Receptor Kinase 1 3
  • BETA-ARK1 3
  • EC 2.7.11 61
  • BARK 4

External Ids for GRK2 Gene

Previous HGNC Symbols for GRK2 Gene

  • ADRBK1

Summaries for GRK2 Gene

Entrez Gene Summary for GRK2 Gene

  • The product of this gene phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization observed at high agonist concentrations. This protein is an ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G-protein-coupled receptors. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart. [provided by RefSeq, Jul 2008]

GeneCards Summary for GRK2 Gene

GRK2 (G Protein-Coupled Receptor Kinase 2) is a Protein Coding gene. Diseases associated with GRK2 include Myocardial Infarction. Among its related pathways are Signaling by GPCR and DAG and IP3 signaling. An important paralog of this gene is GRK3.

UniProtKB/Swiss-Prot for GRK2 Gene

  • 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.

Gene Wiki entry for GRK2 Gene

No data available for Tocris Summary , PharmGKB "VIP" Summary , fRNAdb sequence ontologies and piRNA Summary for GRK2 Gene

Genomics for GRK2 Gene

Regulatory Elements for GRK2 Gene

Enhancers for GRK2 Gene
GeneHancer Identifier Enhancer Score Enhancer Sources Gene-Enhancer Score TSS distance (kb) Number of Genes Away Size (kb) Transcription Factor Binding Sites within enhancer Gene Targets for Enhancer
GH11F067265 1 FANTOM5 ENCODE 13.6 +12.1 12065 25.5 CREB3L1 MLX ZFP64 FEZF1 DMAP1 YBX1 YY1 SLC30A9 ZNF143 ZNF548 SSH3 ENSG00000258297 GRK2 KDM2A ANKRD13D RBM14 PTPRCAP LOC101928069 MRPL11 RHOD
GH11F067316 0.5 ENCODE 12.7 +51.2 51171 2.3 HDGF CREB3L1 WRNIP1 ARID4B SIN3A DMAP1 ZNF2 SLC30A9 ZNF143 ZNF263 CLCF1 MRPL11 LRP5 RHOD GRK2 SSH3 POLD4 RN7SKP239 ENSG00000256514 RNU6-1238P
GH11F067077 1.2 FANTOM5 Ensembl ENCODE 3.7 -188.1 -188059 2.5 TBP KLF17 BRCA1 ZNF366 FOS DEK EGR2 PAF1 SMARCC1 CEBPB RHOD KDM2A ANKRD13D CDK2AP2 GRK2 RBM4 CLCF1 SSH3 TMEM134 PITPNM1
GH11F066949 1.5 FANTOM5 Ensembl ENCODE 2.9 -314.7 -314713 4.3 HDGF PKNOX1 ARID4B SIN3A YY1 ZNF207 FOS DEK ZNF263 SP3 ACTN3 RBM14 ENSG00000258297 LOC105369353 LOC105369352 ENSG00000255038 FAM86C2P RCE1 SYT12 CCS
GH11F066965 1.5 FANTOM5 Ensembl ENCODE 2.6 -297.3 -297348 6.8 ATF1 MLX ARID4B SIN3A DMAP1 ZNF48 BRCA1 YY1 GTF3C2 SLC30A9 RAD9A EIF1AD CLCF1 ENSG00000258297 PC RBM14 RCE1 BRMS1 DPP3 ENSG00000245156
- Elite enhancer/Elite enhancer-gene association Download Table
Download GeneHancer data dump

Enhancers around GRK2 on UCSC Golden Path with GeneCards custom track

Promoters for GRK2 Gene
Ensembl Regulatory Elements (ENSRs) TSS Distance (bp) Size (bp) Binding Sites for Transcription Factors within promoters
ENSR00000189310 900 2601 HDGF PKNOX1 SIN3A ARID4B FEZF1 DMAP1 YY1 GLIS2 ZNF143 FOS

Genomic Location for GRK2 Gene

Chromosome:
11
Start:
67,266,400 bp from pter
End:
67,286,558 bp from pter
Size:
20,159 bases
Orientation:
Plus strand

Genomic View for GRK2 Gene

Genes around GRK2 on UCSC Golden Path with GeneCards custom track

Cytogenetic band:
GRK2 Gene in genomic location: bands according to Ensembl, locations according to GeneLoc (and/or Entrez Gene and/or Ensembl if different)
Genomic Location for GRK2 Gene
GeneLoc Logo Genomic Neighborhood Exon StructureGene Density

RefSeq DNA sequence for GRK2 Gene

Proteins for GRK2 Gene

  • Protein details for GRK2 Gene (UniProtKB/Swiss-Prot)

    Protein Symbol:
    P25098-ARBK1_HUMAN
    Recommended name:
    Beta-adrenergic receptor kinase 1
    Protein Accession:
    P25098
    Secondary Accessions:
    • B0ZBE1
    • Q13837
    • Q6GTT3

    Protein attributes for GRK2 Gene

    Size:
    689 amino acids
    Molecular mass:
    79574 Da
    Quaternary structure:
    • Interacts with GIT1 (By similarity). Interacts with, and phosphorylates chemokine-stimulated CCR5. Interacts with ARRB1. Interacts with LPAR1 and LPAR2. Interacts with RALA in response to LPAR1 activation. ADRBK1 and RALA mutually inhibit each others binding to LPAR1.

    Three dimensional structures from OCA and Proteopedia for GRK2 Gene

neXtProt entry for GRK2 Gene

Selected DME Specific Peptides for GRK2 Gene

P25098:
  • QRVPKMKNKPRSPVVELSK
  • CSHPFSK
  • SVEETQIK
  • ISERWQQEVAETV
  • KFTRFCQWKNVELNIHL
  • YAFHTPDKL
  • YDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDR
  • DVFQKFIES
  • EIKKYEKL
  • VVYRDLK
  • GKDCIMHGYM
  • LGCLGRGAQEVKE
  • FFRSLDW
  • PPRGEVNAADAFDIGSFDEEDTKGIKL
  • EARKKAKNKQL
  • SADWFSLG
  • LPEPSIRSVMQ
  • RISDLGLACDFSKKKPHASVGTHGYMAPEVLQKG
  • GNPFLTQWQRRYFYLFPNRLEWRGE
  • FSPELRSLLEGLLQRDV
  • EIILGLEHMHNRFVVYRDLKPANILLDEHGH
  • GHSPFRQHK
  • LSFILDLMNGGDLHYHLSQHGVFSEADMR
  • QSLLTME
  • DCPFIVCM
  • YMAPEVL
  • LTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCL
  • LFQPYIEEIC
  • LQCDSDPELVQWKKELRD
  • RISDLGLA
  • FILDLMNGGD
  • ILGLEHMH

Post-translational modifications for GRK2 Gene

  • Modification sites at PhosphoSitePlus
  • Modification sites at neXtProt

Other Protein References for GRK2 Gene

ENSEMBL proteins:
REFSEQ proteins:

Antibody Products

  • Cell Signaling Technology (CST) Antibodies for GRK2 (GRK2)
  • Abcam antibodies for GRK2

Domains & Families for GRK2 Gene

Gene Families for GRK2 Gene

Suggested Antigen Peptide Sequences for GRK2 Gene

GenScript: Design optimal peptide antigens:

Graphical View of Domain Structure for InterPro Entry

P25098

UniProtKB/Swiss-Prot:

ARBK1_HUMAN :
  • The PH domain binds anionic phospholipids and helps recruiting ADRBK1 from the cytoplasm to plasma membrane close to activated receptors. It mediates binding to G protein beta and gamma subunits, competing with G-alpha subunits and other G-betagamma effectors.
  • Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily.
Domain:
  • The PH domain binds anionic phospholipids and helps recruiting ADRBK1 from the cytoplasm to plasma membrane close to activated receptors. It mediates binding to G protein beta and gamma subunits, competing with G-alpha subunits and other G-betagamma effectors.
  • Contains 1 AGC-kinase C-terminal domain.
  • Contains 1 PH domain.
  • Contains 1 protein kinase domain.
  • Contains 1 RGS domain.
Family:
  • Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily.
genes like me logo Genes that share domains with GRK2: view

Function for GRK2 Gene

Molecular function for GRK2 Gene

UniProtKB/Swiss-Prot CatalyticActivity:
ATP + [beta-adrenergic receptor] = ADP + [beta-adrenergic receptor] phosphate.
UniProtKB/Swiss-Prot EnzymeRegulation:
In contrast to other AGC family kinases, the catalytic activity is solely regulated by the binding of substrates and ligands, not by phosphorylation of the kinase domain.
UniProtKB/Swiss-Prot 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.

Enzyme Numbers (IUBMB) for GRK2 Gene

Gene Ontology (GO) - Molecular Function for GRK2 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0004672 protein kinase activity IEA,ISS --
GO:0004674 protein serine/threonine kinase activity IEA --
GO:0004703 G-protein coupled receptor kinase activity IEA,ISS --
GO:0005515 protein binding IPI 17006543
GO:0005524 ATP binding IEA --
genes like me logo Genes that share ontologies with GRK2: view
genes like me logo Genes that share phenotypes with GRK2: view

Animal Models for GRK2 Gene

MGI Knock Outs for GRK2:

Animal Model Products

miRNA for GRK2 Gene

miRTarBase miRNAs that target GRK2

Inhibitory RNA Products

Clone Products

  • Addgene plasmids for GRK2

Flow Cytometry Products

No data available for Human Phenotype Ontology , Transcription Factor Targets and HOMER Transcription for GRK2 Gene

Localization for GRK2 Gene

Subcellular locations from UniProtKB/Swiss-Prot for GRK2 Gene

Cytoplasm. Cell membrane.

Gene Ontology (GO) - Cellular Components for GRK2 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005737 cytoplasm IEA,IDA 17986524
GO:0005829 cytosol TAS --
GO:0005886 plasma membrane IEA,TAS --
GO:0016020 membrane ISS --
genes like me logo Genes that share ontologies with GRK2: view

No data available for Subcellular locations from COMPARTMENTS for GRK2 Gene

Pathways & Interactions for GRK2 Gene

genes like me logo Genes that share pathways with GRK2: view

SIGNOR curated interactions for GRK2 Gene

Activates:
Inactivates:
Is activated by:
Is inactivated by:
Other effect:

Gene Ontology (GO) - Biological Process for GRK2 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0002026 regulation of the force of heart contraction IEA --
GO:0002029 desensitization of G-protein coupled receptor protein signaling pathway IEA,ISS --
GO:0003108 negative regulation of the force of heart contraction by chemical signal IMP 15051637
GO:0006468 protein phosphorylation IEA --
GO:0007165 signal transduction IEA --
genes like me logo Genes that share ontologies with GRK2: view

Drugs & Compounds for GRK2 Gene

(30) Drugs for GRK2 Gene - From: DrugBank, HMDB, and Novoseek

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
Adenosine triphosphate Approved Nutra Target 0
Zinc Approved Pharma 2231

(25) Additional Compounds for GRK2 Gene - From: Novoseek, Tocris, and HMDB

Name Synonyms Role CAS Number PubChem IDs PubMed IDs
ADP
  • Adenosindiphosphorsaeure
  • Adenosine 5'-pyrophosphate
  • Adenosine diphosphate
  • Adenosine pyrophosphate
  • Adenosine-5'-diphosphate
Full agonist, Agonist 58-64-0
8-Bromo-cGMP, sodium salt
51116-01-9
CMPD101
865608-11-3
Gallein
2103-64-2
G-Protein antagonist peptide
143675-79-0

(5) Tocris Compounds for GRK2 Gene

Compound Action Cas Number
8-Bromo-cGMP, sodium salt cGMP analog; activates PKG 51116-01-9
CMPD101 Potent and selective GRK2/3 inhibitor 865608-11-3
Gallein Inhibitor of betagamma signaling 2103-64-2
G-Protein antagonist peptide Inhibits G protein activation by GPCRs 143675-79-0
Pertussis Toxin Catalyzes ADP-ribosylation of Gi, Go and Gt 70323-44-3
genes like me logo Genes that share compounds with GRK2: view

Transcripts for GRK2 Gene

Unigene Clusters for GRK2 Gene

Adrenergic, beta, receptor kinase 1:
Representative Sequences:

Inhibitory RNA Products

Clone Products

  • Addgene plasmids for GRK2

Flow Cytometry Products

Alternative Splicing Database (ASD) splice patterns (SP) for GRK2 Gene

No ASD Table

Relevant External Links for GRK2 Gene

GeneLoc Exon Structure for
GRK2
ECgene alternative splicing isoforms for
GRK2

Expression for GRK2 Gene

NURSA nuclear receptor signaling pathways regulating expression of GRK2 Gene:

GRK2

SOURCE GeneReport for Unigene cluster for GRK2 Gene:

Hs.83636

mRNA Expression by UniProt/SwissProt for GRK2 Gene:

P25098-ARBK1_HUMAN
Tissue specificity: Expressed in peripheral blood leukocytes.

Primer Products

No data available for mRNA expression in normal human tissues , mRNA expression in embryonic tissues and stem cells from LifeMap Discovery , mRNA differential expression in normal tissues , Protein differential expression in normal tissues , Protein expression and Protein tissue co-expression partners for GRK2 Gene

Orthologs for GRK2 Gene

This gene was present in the common ancestor of animals.

Orthologs for GRK2 Gene

Organism Taxonomy Gene Similarity Type Details
chimpanzee
(Pan troglodytes)
Mammalia ADRBK1 34 35
  • 99.61 (n)
platypus
(Ornithorhynchus anatinus)
Mammalia ADRBK1 35
  • 95 (a)
OneToOne
cow
(Bos Taurus)
Mammalia ADRBK1 34 35
  • 93.03 (n)
dog
(Canis familiaris)
Mammalia ADRBK1 34 35
  • 92.74 (n)
rat
(Rattus norvegicus)
Mammalia Adrbk1 34
  • 90.32 (n)
mouse
(Mus musculus)
Mammalia Adrbk1 34 16 35
  • 89.85 (n)
chicken
(Gallus gallus)
Aves ADRBK1 34 35
  • 85.42 (n)
lizard
(Anolis carolinensis)
Reptilia ADRBK1 35
  • 92 (a)
OneToOne
zebrafish
(Danio rerio)
Actinopterygii adrbk2 35
  • 85 (a)
OneToMany
fruit fly
(Drosophila melanogaster)
Insecta Gprk1 35
  • 65 (a)
OneToMany
worm
(Caenorhabditis elegans)
Secernentea grk-2 35
  • 64 (a)
OneToMany
sea squirt
(Ciona savignyi)
Ascidiacea CSA.9837 35
  • 59 (a)
ManyToMany
Species where no ortholog for GRK2 was found in the sources mined by GeneCards:
  • A. gosspyii yeast (Ashbya gossypii)
  • Actinobacteria (Mycobacterium tuberculosis)
  • African clawed frog (Xenopus laevis)
  • African malaria mosquito (Anopheles gambiae)
  • Alicante grape (Vitis vinifera)
  • alpha proteobacteria (Wolbachia pipientis)
  • amoeba (Dictyostelium discoideum)
  • Archea (Pyrococcus horikoshii)
  • baker's yeast (Saccharomyces cerevisiae)
  • barley (Hordeum vulgare)
  • beta proteobacteria (Neisseria meningitidis)
  • bread mold (Neurospora crassa)
  • Chromalveolata (Phytophthora infestans)
  • common water flea (Daphnia pulex)
  • corn (Zea mays)
  • E. coli (Escherichia coli)
  • filamentous fungi (Aspergillus nidulans)
  • Firmicute bacteria (Streptococcus pneumoniae)
  • fission yeast (Schizosaccharomyces pombe)
  • green algae (Chlamydomonas reinhardtii)
  • honey bee (Apis mellifera)
  • K. lactis yeast (Kluyveromyces lactis)
  • loblloly pine (Pinus taeda)
  • malaria parasite (Plasmodium falciparum)
  • medicago trunc (Medicago Truncatula)
  • moss (Physcomitrella patens)
  • oppossum (Monodelphis domestica)
  • orangutan (Pongo pygmaeus)
  • pig (Sus scrofa)
  • rainbow trout (Oncorhynchus mykiss)
  • rice (Oryza sativa)
  • rice blast fungus (Magnaporthe grisea)
  • schistosome parasite (Schistosoma mansoni)
  • sea anemone (Nematostella vectensis)
  • sea urchin (Strongylocentrotus purpuratus)
  • sorghum (Sorghum bicolor)
  • soybean (Glycine max)
  • stem rust fungus (Puccinia graminis)
  • sugarcane (Saccharum officinarum)
  • thale cress (Arabidopsis thaliana)
  • tomato (Lycopersicon esculentum)
  • toxoplasmosis (Toxoplasma gondii)
  • Trichoplax (Trichoplax adhaerens)
  • tropical clawed frog (Silurana tropicalis)
  • wheat (Triticum aestivum)

Evolution for GRK2 Gene

ENSEMBL:
Gene Tree for GRK2 (if available)
TreeFam:
Gene Tree for GRK2 (if available)

Paralogs for GRK2 Gene

Paralogs for GRK2 Gene

genes like me logo Genes that share paralogs with GRK2: view

Variants for GRK2 Gene

Sequence variations from dbSNP and Humsavar for GRK2 Gene

SNP ID Clin Chr 11 pos Sequence Context AA Info Type
VAR_040379 A colorectal adenocarcinoma sample
rs1009943 -- 67,281,168(+) GGAAG(C/G)CTGAC nc-transcript-variant, reference, missense
rs1009944 -- 67,281,169(+) GAAGG(C/G)TGACA nc-transcript-variant, reference, missense
rs1051180 -- 67,283,165(+) ACTAC(A/G)CTCCC nc-transcript-variant, reference, missense
rs1051181 -- 67,284,908(+) CCCTT(C/T)CTGAC nc-transcript-variant, reference, synonymous-codon

Structural Variations from Database of Genomic Variants (DGV) for GRK2 Gene

Variant ID Type Subtype PubMed ID
nsv1118215 CNV deletion 24896259
nsv468603 CNV loss 19166990
nsv555253 CNV loss 21841781
nsv951021 CNV deletion 24416366

Variation tolerance for GRK2 Gene

Residual Variation Intolerance Score: 2.58% of all genes are more intolerant (likely to be disease-causing)
Gene Damage Index Score: 1.06; 21.66% of all genes are more intolerant (likely to be disease-causing)

Relevant External Links for GRK2 Gene

SNPedia medical, phenotypic, and genealogical associations of SNPs for
GRK2

No data available for Polymorphic Variants from UniProtKB/Swiss-Prot for GRK2 Gene

Disorders for GRK2 Gene

MalaCards: The human disease database

(1) MalaCards diseases for GRK2 Gene - From: DISEASES, Novoseek, and GeneCards

Disorder Aliases PubMed IDs
myocardial infarction
  • myocardial infarction, protection against
- elite association - COSMIC cancer census association via MalaCards
Search GRK2 in MalaCards View complete list of genes associated with diseases

Relevant External Links for GRK2

Atlas of Genetics and Cytogenetics in Oncology and Haematology:
GRK2
genes like me logo Genes that share disorders with GRK2: view

No data available for UniProtKB/Swiss-Prot and Genatlas for GRK2 Gene

Publications for GRK2 Gene

  1. Monocyte chemoattractant protein-1-induced CCR2B receptor desensitization mediated by the G protein-coupled receptor kinase 2. (PMID: 9501202) Aragay A.M. … Mayor F. Jr. (Proc. Natl. Acad. Sci. U.S.A. 1998) 3 4 22 64
  2. cDNA cloning and chromosomal localization of the human beta- adrenergic receptor kinase. (PMID: 2037065) Benovic J.L. … Lefkowitz R.J. (FEBS Lett. 1991) 2 3 4 64
  3. [High glucose up-regulates GRK2 gene expression in H9C2 cardiomyoblasts in vitro]. (PMID: 20335112) Chen H.M. … Yu X.Y. (Nan Fang Yi Ke Da Xue Xue Bao 2010) 3 22 64
  4. G protein-coupled receptor kinase 2 (GRK2) modulation and cell cycle progression. (PMID: 20080565) Penela P. … Mayor F. (Proc. Natl. Acad. Sci. U.S.A. 2010) 3 22 64
  5. Dynamic changes in lymphocyte GRK2 levels in cardiac transplant patients: a biomarker for left ventricular function. (PMID: 20443948) Bonita R.E. … Koch W.J. (Clin Transl Sci 2010) 3 22 64

Products for GRK2 Gene

Sources for GRK2 Gene

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