GRK2
Summary: 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].
| Name | OMIM ID | Ensembl ID | HGNC ID | PHARMGKB ID | Map Location |
|---|---|---|---|---|---|
| G protein-coupled receptor kinase 2 | MIM:109635 | Ensembl:ENSG00000173020 | HGNC:HGNC:289 | PA40 | 11q13.2 |
GO terms in GRK2
| Term Type | Evidence Type | GO Term ID | GO Des. |
|---|---|---|---|
| BP | ISS | GO:0002029 | desensitization of G-protein coupled receptor protein signaling pathway |
| BP | IMP | GO:0003108 | negative regulation of the force of heart contraction by chemical signal |
| BP | TAS | GO:0007186 | G-protein coupled receptor signaling pathway |
| BP | ISS | GO:0007213 | G-protein coupled acetylcholine receptor signaling pathway |
| BP | IDA | GO:0007217 | tachykinin receptor signaling pathway |
| BP | IEA | GO:0007507 | heart development |
| BP | ISS | GO:0018105 | peptidyl-serine phosphorylation |
| BP | IEA | GO:0018107 | peptidyl-threonine phosphorylation |
| BP | IMP | GO:0019079 | viral genome replication |
| BP | IDA | GO:0031623 | receptor internalization |
| BP | ISS | GO:0033605 | positive regulation of catecholamine secretion |
| BP | IMP | GO:0045988 | negative regulation of striated muscle contraction |
| BP | IMP | GO:0046718 | viral entry into host cell |
| BP | IMP | GO:0060048 | cardiac muscle contraction |
| CC | IDA | GO:0005737 | cytoplasm |
| CC | TAS | GO:0005829 | cytosol |
| CC | TAS | GO:0005886 | plasma membrane |
| CC | TAS | GO:0005929 | cilium |
| CC | HDA | GO:0016020 | membrane |
| CC | ISS | GO:0016020 | membrane |
| MF | ISS | GO:0004672 | protein kinase activity |
| MF | ISS | GO:0004703 | G-protein coupled receptor kinase activity |
| MF | IPI | GO:0005515 | protein binding |
| MF | IEA | GO:0005524 | ATP binding |
| MF | ISS | GO:0031694 | alpha-2A adrenergic receptor binding |
| MF | IDA | GO:0031755 | Edg-2 lysophosphatidic acid receptor binding |
| MF | TAS | GO:0047696 | beta-adrenergic receptor kinase activity |
Gene expression in normal tissue: GRK2
Gene-model tissue-cancer distribution: Bubble Plot
Gene-drug pathway distribution
Pathways in GRK2
| Database | Pathway ID | Pathway Des. |
|---|---|---|
| biocarta | barrestinpathway | -arrestins in gpcr desensitization |
| biocarta | barrestinsrcpathway | roles of arrestin dependent recruitment of src kinases in gpcr signaling |
| biocarta | barrmapkpathway | role of -arrestins in the activation and targeting of map kinases |
| biocarta | ck1pathway | regulation of ck1/cdk5 by type 1 glutamate receptors |
| reactome | R-HSA-111885 | Opioid Signalling |
| reactome | R-HSA-111933 | Calmodulin induced events |
| reactome | R-HSA-111996 | Ca-dependent events |
| reactome | R-HSA-111997 | CaM pathway |
| reactome | R-HSA-112040 | G-protein mediated events |
| reactome | R-HSA-112043 | PLC beta mediated events |
| reactome | R-HSA-1489509 | DAG and IP3 signaling |
| reactome | R-HSA-162582 | Signal Transduction |
| reactome | R-HSA-162582 | Signal Transduction |
| reactome | R-HSA-199991 | Membrane Trafficking |
| reactome | R-HSA-372790 | Signaling by GPCR |
| reactome | R-HSA-388396 | GPCR downstream signalling |
| reactome | R-HSA-416476 | G alpha (q) signalling events |
| reactome | R-HSA-418555 | G alpha (s) signalling events |
| reactome | R-HSA-418594 | G alpha (i) signalling events |
| reactome | R-HSA-5358351 | Signaling by Hedgehog |
| reactome | R-HSA-5358351 | Signaling by Hedgehog |
| reactome | R-HSA-5632684 | Hedgehog 'on' state |
| reactome | R-HSA-5632684 | Hedgehog 'on' state |
| reactome | R-HSA-5635838 | Activation of SMO |
| reactome | R-HSA-5635838 | Activation of SMO |
| reactome | R-HSA-5653656 | Vesicle-mediated transport |
| reactome | R-HSA-8856825 | Cargo recognition for clathrin-mediated endocytosis |
| reactome | R-HSA-8856828 | Clathrin-mediated endocytosis |
| reactome | R-HSA-9006925 | Intracellular signaling by second messengers |
| wikipathways | WP3929 | Chemokine signaling pathway |
| wikipathways | WP4249 | Hedgehog Signaling Pathway |
| wikipathways | WP47 | Hedgehog Signaling Pathway |
| pid | cxcr4_pathway | CXCR4-mediated signaling events |
| pid | hdac_classii_pathway | Signaling events mediated by HDAC Class II |
| pid | hedgehog_2pathway | Signaling events mediated by the Hedgehog family |
| pid | il8cxcr1_pathway | IL8- and CXCR1-mediated signaling events |
| pid | txa2pathway | Thromboxane A2 receptor signaling |
| pharmgkb | PA165984799 | Diuretics Pathway, Pharmacodynamics |
| pharmgkb | PA2024 | Beta-agonist/Beta-blocker Pathway, Pharmacodynamics |
| kegg | hsa04062 | Chemokine signaling pathway - Homo sapiens (human) |
| kegg | hsa04144 | Endocytosis - Homo sapiens (human) |
| kegg | hsa04340 | Hedgehog signaling pathway - Homo sapiens (human) |
| kegg | hsa04724 | Glutamatergic synapse - Homo sapiens (human) |
| kegg | hsa04740 | Olfactory transduction - Homo sapiens (human) |
| kegg | hsa05032 | Morphine addiction - Homo sapiens (human) |
| netpath | Pathway_EGFR1 | EGFR1 |
| netpath | Pathway_Hedgehog | Hedgehog |
Gene-Drug: Aster Plot
| Drug ID | Drug Name | Model Num. |
|---|---|---|
| iGMDRD286 | Nsc 632839 | 3 |
| iGMDRD414 | MST-312 | 3 |
| iGMDRD152 | 179324-69-7 | 3 |
| iGMDRD237 | ABT-751 | 3 |
| iGMDRD577 | BIX01294 | 3 |
| iGMDRD394 | BX-795 | 2 |
| iGMDRD280 | CYTOCHALASIN B | 6 |
| iGMDRD945 | ML214 | 2 |
| iGMDRD158 | NSC141540 | 2 |
| iGMDRD271 | Brefeldin A | 1 |
| iGMDRD512 | nutlin 3 | 3 |
| iGMDRD105 | Triptolide | 6 |
| iGMDRD289 | Parthenolide | 1 |
| iGMDRD77 | Itraconazole | 3 |
Gene in drug-gene network: Network Plot
Gene-drug targets distribution
Gene Structure: PDB
Models in GRK2
CLASSFICATION
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