Target Information

Target General Infomation
Target ID
T62548
Former ID
TTDR00280
Target Name
Beta-adrenergic receptor kinase 1
Gene Name
GRK2
Synonyms
Beta ARK1; Beta-ARK-1; BetaARK1; G-protein coupled receptor kinase 2; GRK2
Target Type
Research
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.
BioChemical Class
Kinase
UniProt ID
P25098
EC Number
EC 2.7.11.15
Sequence
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFS
QKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLAC
SHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNV
ELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNER
IMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAE
IILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPE
VLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAA
DAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARK
KAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSL
LTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQR
VPKMKNKPRSPVVELSKVPLVQRGSANGL
Inhibitor BetaARKct Drug Info [535312]
compound 101 Drug Info [531490]
compound 1o Drug Info [532542]
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 531490Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors. Mol Pharmacol. 2011 Aug;80(2):294-303.
Ref 532542Design 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.
Ref 535312Gene-mediated inhibition of the b-adrenergic receptor kinase: a new therapeutic strategy for heart failure. Minerva Cardioangiol. 2001 Dec;49(6):389-94.

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