Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T62548
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| Former ID |
TTDR00280
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| Target Name |
Beta-adrenergic receptor kinase 1
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| Gene Name |
GRK2
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| Synonyms |
Beta ARK1; Beta-ARK-1; BetaARK1; G-protein coupled receptor kinase 2; GRK2
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| Target Type |
Research
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| 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.
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| BioChemical Class |
Kinase
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| UniProt ID | |||||
| EC Number |
EC 2.7.11.15
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| Sequence |
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR VPKMKNKPRSPVVELSKVPLVQRGSANGL |
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| Inhibitor | BetaARKct | Drug Info | [1] | ||
| compound 101 | Drug Info | [2] | |||
| compound 1o | Drug Info | [3] | |||
| Pathways | |||||
| KEGG Pathway | Chemokine signaling pathway | ||||
| Endocytosis | |||||
| Glutamatergic synapse | |||||
| Morphine addiction | |||||
| PANTHER Pathway | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | ||||
| Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway | |||||
| Parkinson disease | |||||
| Angiotensin II-stimulated signaling through G proteins and beta-arrestin | |||||
| Pathway Interaction Database | Signaling events mediated by HDAC Class II | ||||
| Thromboxane A2 receptor signaling | |||||
| CXCR4-mediated signaling events | |||||
| Signaling events mediated by the Hedgehog family | |||||
| IL8- and CXCR1-mediated signaling events | |||||
| Reactome | Calmodulin induced events | ||||
| G alpha (q) signalling events | |||||
| Activation of SMO | |||||
| WikiPathways | Hedgehog Signaling Pathway | ||||
| DAG and IP3 signaling | |||||
| Gastrin-CREB signalling pathway via PKC and MAPK | |||||
| Opioid Signalling | |||||
| GPCR downstream signaling | |||||
| References | |||||
| REF 1 | Gene-mediated inhibition of the b-adrenergic receptor kinase: a new therapeutic strategy for heart failure. Minerva Cardioangiol. 2001 Dec;49(6):389-94. | ||||
| REF 2 | Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol Pharmacol. 2011 Aug;80(2):294-303. | ||||
| REF 3 | Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6711-6. | ||||
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