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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 56
  • 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 56
  • BARK 4

External Ids for GRK2 Gene

Previous HGNC Symbols for GRK2 Gene

  • ADRBK1

Summaries for GRK2 Gene

Entrez Gene Summary for GRK2 Gene

  • This gene encodes a member of the G protein-coupled receptor kinase family of proteins. The encoded protein phosphorylates the beta-adrenergic receptor as well as a wide range of other substrates including non-GPCR cell surface receptors, and cytoskeletal, mitochondrial, and transcription factor proteins. Data from rodent models supports a role for this gene in embryonic development, heart function and metabolism. Elevated expression of this gene has been observed in human patients with heart failure and Alzheimer's disease. [provided by RefSeq, Sep 2017]

GeneCards Summary for GRK2 Gene

GRK2 (G Protein-Coupled Receptor Kinase 2) is a Protein Coding gene. Diseases associated with GRK2 include Heart Disease and Alzheimer Disease. Among its related pathways are DAG and IP3 signaling and Circadian entrainment. 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

Additional gene information for GRK2 Gene

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

Genomics for GRK2 Gene

GeneHancer (GH) Regulatory Elements for GRK2 Gene

Promoters and enhancers for GRK2 Gene
GeneHancer (GH) Identifier GH Type GH
Score
GH Sources Gene Association Score Total Score TSS distance (kb) Number of Genes Away Size (kb) Transcription Factor
Binding Sites
Gene Targets
GH11I067265 Promoter/Enhancer 2.6 EPDnew FANTOM5 Ensembl ENCODE dbSUPER 563.7 +12.1 12064 25.5 HDGF PKNOX1 CLOCK SMAD1 FOXA2 MLX ARID4B SIN3A DMAP1 ZNF2 GRK2 ANKRD13D SSH3 KDM2A PTPRCAP RHOD CARNS1 C11orf80 PC RAD9A
GH11I067264 Enhancer 0.4 FANTOM5 dbSUPER 550.8 -1.4 -1363 0.1 GRK2 PIR33652
GH11I067316 Promoter/Enhancer 1.6 Ensembl ENCODE 12.8 +51.2 51171 2.3 HDGF SMAD1 ARID4B SIN3A DMAP1 ZNF2 YY1 SLC30A9 POLR2B ZNF213 LOC100130987 RAD9A SSH3 ENSG00000258297 RBM4 KMT5B RBM14 GRK2 UNC93B1 POLD4
GH11I067077 Enhancer 1.5 FANTOM5 Ensembl ENCODE dbSUPER 3.7 -188.1 -188059 2.5 HDAC1 CLOCK SREBF2 NEUROD1 KLF17 BATF BRCA1 EGR1 ZNF366 FOS RHOD KDM2A ANKRD13D CDK2AP2 GRK2 RBM4 CLCF1 SSH3 TMEM134 PITPNM1
GH11I066949 Enhancer 1.7 FANTOM5 Ensembl ENCODE dbSUPER 2.9 -314.7 -314713 4.3 HDGF PKNOX1 ARID4B SIN3A YY1 FOS DEK SP3 ZHX2 SMARCB1 ACTN3 ENSG00000258297 SYT12 RBM14 ENSG00000254461 RHOD RPS6KB2 LOC101928069 CLCF1 GRK2
- Elite GeneHancer and/or Elite GeneHancer-gene association Download GeneHancer data dump

GeneHancers around GRK2 on UCSC Golden Path with GeneCards custom track

Genomic Locations for GRK2 Gene

Genomic Locations for GRK2 Gene
chr11:67,266,400-67,286,558
(GRCh38/hg38)
Size:
20,159 bases
Orientation:
Plus strand
chr11:67,033,881-67,054,029
(GRCh37/hg19)

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

No Post-translational modifications

Other Protein References for GRK2 Gene

ENSEMBL proteins:
REFSEQ proteins:

Domains & Families for GRK2 Gene

Gene Families for GRK2 Gene

HGNC:
Human Protein Atlas (HPA):
  • Enzymes
  • Plasma proteins
  • Predicted intracellular proteins

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.
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

Phenotypes From GWAS Catalog 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

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.

Subcellular locations from

COMPARTMENTS
Extracellular space Cytosol Plasma membrane Cytoskeleton Lysosome Endosome Peroxisome ER Golgi Apparatus Nucleus Mitochondrion 0 1 2 3 4 5 Confidence
COMPARTMENTS Subcellular localization image for GRK2 gene
Compartment Confidence
plasma membrane 5
cytosol 5
mitochondrion 2
nucleus 2
endosome 2
extracellular 1
cytoskeleton 1
endoplasmic reticulum 1

Subcellular locations from the

Human Protein Atlas (HPA)

Gene Ontology (GO) - Cellular Components for GRK2 Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005737 cytoplasm IDA,IEA 17986524
GO:0005829 cytosol TAS --
GO:0005886 plasma membrane TAS --
GO:0005929 cilium TAS --
GO:0016020 membrane ISS --
genes like me logo Genes that share ontologies with GRK2: view

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

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

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
Zinc Approved, Investigational Pharma 2430
ATP Investigational Nutra Agonist, Target 0

(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
G-Protein antagonist peptide
143675-79-0

(5) Tocris Compounds for GRK2 Gene

Compound Action Cas Number
[D-Trp7,9,10]-Substance P Inhibits M1 ACh receptor activation of Gq/11 89430-38-6
G-Protein antagonist peptide Inhibits G protein activation by GPCRs 143675-79-0
Gue 1654 Selective inhibitor of OXE-R Gbetagamma signaling 397290-30-1
Mastoparan Activates Gi and Go 72093-21-1
SCH 202676 hydrobromide Inhibitor of ligand binding to G-protein-coupled receptors 265980-25-4
genes like me logo Genes that share compounds with GRK2: view

Transcripts for GRK2 Gene

Inhibitory RNA Products

Clone Products

  • Addgene plasmids for GRK2

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

mRNA Expression by UniProt/SwissProt for GRK2 Gene:

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

Evidence on tissue expression from TISSUES for GRK2 Gene

  • Blood(4.7)
  • Nervous system(4.7)
  • Heart(3)
  • Muscle(2.9)
  • Intestine(2.8)
  • Lung(2.7)
  • Kidney(2.6)
  • Bone marrow(2.2)
  • Adrenal gland(2.1)
  • Lymph node(2)

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 , Protein tissue co-expression partners and Phenotype-based relationships between genes and organs from Gene ORGANizer 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 33 34
  • 99.61 (n)
platypus
(Ornithorhynchus anatinus)
Mammalia ADRBK1 34
  • 95 (a)
OneToOne
cow
(Bos Taurus)
Mammalia ADRBK1 33 34
  • 93.03 (n)
dog
(Canis familiaris)
Mammalia ADRBK1 33 34
  • 92.74 (n)
rat
(Rattus norvegicus)
Mammalia Adrbk1 33
  • 90.32 (n)
mouse
(Mus musculus)
Mammalia Adrbk1 33 34
  • 89.85 (n)
Grk2 16
chicken
(Gallus gallus)
Aves ADRBK1 33 34
  • 85.42 (n)
lizard
(Anolis carolinensis)
Reptilia ADRBK1 34
  • 92 (a)
OneToOne
zebrafish
(Danio rerio)
Actinopterygii adrbk2 34
  • 85 (a)
OneToMany
fruit fly
(Drosophila melanogaster)
Insecta Gprk1 34
  • 65 (a)
OneToMany
worm
(Caenorhabditis elegans)
Secernentea grk-2 34
  • 64 (a)
OneToMany
sea squirt
(Ciona savignyi)
Ascidiacea CSA.9837 34
  • 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 Variation AA Info Type
VAR_040379 A colorectal adenocarcinoma sample p.Arg578Gln
rs1000454302 -- 67,277,568(+) C/T intron_variant
rs1000570063 -- 67,278,372(+) G/A intron_variant
rs1000623837 -- 67,278,726(+) T/C intron_variant
rs1000807718 -- 67,284,523(+) G/A intron_variant

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

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

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)

Additional Variant Information 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

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

Disorder Aliases PubMed IDs
heart disease
  • congenital heart disease
alzheimer disease
  • ad
myocardial infarction
  • myocardial infarction, susceptibility to
- elite association - COSMIC cancer census association via MalaCards
Search GRK2 in MalaCards View complete list of genes associated with diseases

Additional Disease Information for 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 AM … Mayor F (Proceedings of the National Academy of Sciences of the United States of America 1998) 3 4 22 58
  2. cDNA cloning and chromosomal localization of the human beta-adrenergic receptor kinase. (PMID: 2037065) Benovic JL … Lefkowitz RJ (FEBS letters 1991) 2 3 4 58
  3. G protein-coupled receptor kinase 2 (GRK2) modulation and cell cycle progression. (PMID: 20080565) Penela P … Mayor F (Proceedings of the National Academy of Sciences of the United States of America 2010) 3 22 58
  4. [High glucose up-regulates GRK2 gene expression in H9C2 cardiomyoblasts in vitro]. (PMID: 20335112) Chen HM … Yu XY (Nan fang yi ke da xue xue bao = Journal of Southern Medical University 2010) 3 22 58
  5. Dynamic changes in lymphocyte GRK2 levels in cardiac transplant patients: a biomarker for left ventricular function. (PMID: 20443948) Bonita RE … Koch WJ (Clinical and translational science 2010) 3 22 58

Products for GRK2 Gene

Sources for GRK2 Gene

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