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GeneE
10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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GRK6
G protein-coupled receptor kinase 6
Chromosome 5 · 5q35.3
NCBI Gene: 2870Ensembl: ENSG00000198055.12HGNC: HGNC:4545UniProt: B3KPS5
93PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Kinase
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
beta-adrenergic receptor kinase activitydesensitization of G protein-coupled receptor signaling pathwayprotein bindingmembranecongenital factor XII deficiencyhereditary angioedema type 3neurodegenerative diseasehypertension
✦AI Summary

GRK6 (G protein-coupled receptor kinase 6) is a serine/threonine kinase that phosphorylates activated G protein-coupled receptors (GPCRs), initiating β-arrestin-mediated receptor desensitization and internalization 1. The enzyme localizes to the plasma membrane and cytoplasm, where it regulates GPCR signaling pathway termination through phosphorylation of agonist-occupied receptors 2. GRK6 contains an AGC kinase domain, though hypoxia can promote expression of truncated isoforms lacking this domain 3. Post-translational palmitoylation of GRK6 is critical for its membrane translocation and activation of downstream signaling cascades. In triple-negative breast cancer (TNBC), GRK6 upregulation correlates with increased metastatic potential through activation of the β-Arrestin 2/MAPK/NF-κB axis, and GRK6 inhibition suppresses migration 1. Conversely, in lung adenocarcinoma, GRK6 is downregulated through promoter hypermethylation, with reduced expression promoting cell migration and invasion via altered E-cadherin/vimentin expression and increased matrix metalloproteinases 4. In pulmonary arterial hypertension, GRK6 overexpression provides protective effects by attenuating smooth muscle cell proliferation through STAT3 pathway inhibition 5. In inflammatory responses, GRK6 palmitoylation-dependent membrane translocation promotes PI3K/AKT signaling and inflammatory mediator release 6. These findings demonstrate context-dependent roles for GRK6 in cancer progression, cardiovascular disease, and inflammation.

Sources cited
1
GRK6 upregulation in TNBC correlates with metastasis; palmitoylation activates β-Arrestin 2/MAPK/NF-κB axis; GRK6 inhibition suppresses migration
PMID: 39741338
2
Hypoxia increases expression of truncated GRK6 isoform lacking AGC kinase domain in breast cancer cells
PMID: 38906680
3
GRK6 localizes to chromosome 5; phosphorylates agonist-occupied GPCRs causing desensitization; contains introns and produces multiple transcripts
PMID: 9016947
4
GRK6 is downregulated in lung adenocarcinoma via promoter hypermethylation; GRK6 knockdown promotes migration/invasion; overexpression increases E-cadherin and decreases MMP2/7
PMID: 30984536
5
GRK6 overexpression protects against pulmonary arterial hypertension by inhibiting STAT3 phosphorylation and smooth muscle cell proliferation
PMID: 37742818
6
GRK6 palmitoylation promotes membrane translocation and activates PI3K/AKT signaling in LPS-induced Kupffer cell inflammation
PMID: 37012861
7
GRK6 is upregulated in colorectal carcinoma and correlates with poor survival, lymph node invasion, distant metastasis, and advanced TNM stage
PMID: 29552218
8
GRK6 undergoes autophosphorylation on Ser484 and Thr485 in cells; catalytic activity not required for some GPCR phosphorylation events
PMID: 10334944
Disease Associationsⓘ20
congenital factor XII deficiencyOpen Targets
0.52Moderate
hereditary angioedema type 3Open Targets
0.51Moderate
neurodegenerative diseaseOpen Targets
0.42Moderate
hypertensionOpen Targets
0.35Weak
hereditary angioedemaOpen Targets
0.34Weak
angioedemaOpen Targets
0.34Weak
HyperbilirubinemiaOpen Targets
0.34Weak
hypertensive disorderOpen Targets
0.34Weak
urticariaOpen Targets
0.34Weak
Parkinson diseaseOpen Targets
0.25Weak
multiple sclerosisOpen Targets
0.24Weak
Alzheimer diseaseOpen Targets
0.24Weak
lysosomal storage diseaseOpen Targets
0.24Weak
genetic disorderOpen Targets
0.19Weak
thrombotic diseaseOpen Targets
0.12Weak
intelligenceOpen Targets
0.11Weak
hypothyroidismOpen Targets
0.10Weak
vascular diseaseOpen Targets
0.10Weak
triple-negative breast cancerOpen Targets
0.08Suggestive
TinnitusOpen Targets
0.07Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
GIT1Protein interaction100%GIT2Protein interaction100%CXCR4Protein interaction96%ADRB2Protein interaction92%CXCR1Protein interaction79%CXCR2Protein interaction78%
Tissue Expression6 tissues
Bone Marrow
100%
Lung
47%
Brain
19%
Ovary
18%
Liver
18%
Heart
17%
Gene Interaction Network
Click a node to explore
GRK6GIT1GIT2CXCR4ADRB2CXCR1CXCR2
PROTEIN STRUCTURE
Preparing viewer…
PDB2ACX · 2.60 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.60LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF0.46 [0.35–0.60]
RankingsWhere GRK6 stands among ~20K protein-coding genes
  • #5,141of 20,598
    Most Researched93 · top quartile
  • #4,163of 17,882
    Most Constrained (LOEUF)0.60 · top quartile
Genes detectedGRK6
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Long-read Ribo-STAMP simultaneously measures transcription and translation with isoform resolution.
PMID: 38906680
Genome Res · 2024
1.00
2
GRK6 palmitoylation dictates triple-negative breast cancer metastasis via recruiting the β-Arrestin 2/MAPKs/NF-κB signaling axis.
PMID: 39741338
Breast Cancer Res · 2024
0.90
3
Identification and chromosomal localization of a processed pseudogene of human GRK6.
PMID: 9016947
Gene · 1997
0.80
4
Therapeutic potential and protective role of GRK6 overexpression in pulmonary arterial hypertension.
PMID: 37742818
Vascul Pharmacol · 2023
0.70
5
Hypermethylation of the G protein-coupled receptor kinase 6 (GRK6) promoter inhibits binding of C/EBPα, and GRK6 knockdown promotes cell migration and invasion in lung adenocarcinoma cells.
PMID: 30984536
FEBS Open Bio · 2019
0.60