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Tchem
GRK2
Beta-adrenergic receptor kinase 1

Protein Summary
Description
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 (PubMed:19306925, PubMed:19715378). Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by faciltating the trafficking of SMO into the cilium and the stimulation of SMO activity (By similarity). 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 ...more
Uniprot Accession IDs
Gene Name
Ensembl ID
  • ENST00000308595
  • ENSP00000312262
  • ENSG00000173020

Symbol
  • ADRBK1
  • BARK
  • BARK1
  • BARK1
  • ADRBK1
  • BETA-ARK1
Illumination Graph
Knowledge Table
Most Knowledge About
Knowledge Value (0 to 1 scale)
biological process
0
biological term
0
cell line
0
cell type or tissue
0
cellular component
0


IDG Development Level Summary
Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 463.81   (req: < 5)
Gene RIFs: 139   (req: <= 3)
Antibodies: 626   (req: <= 50)
Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 463.81   (req: >= 5)
Gene RIFs: 139   (req: > 3)
Antibodies: 626   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 20
Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 42
Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0
Protein Data Bank (16)
1 – 5 of 16
PDB Structure Id
Ligand
Method
Resolution (Å)
M.W. (kDa)
Pub Year
Title
PDB Structure Id
M.W.
Resolution
Pub Year
Pathways (48)
Activation of SMO (R-HSA-5635838)

Click on a row in the table to change the structure displayed.

Items per page:
1 – 5 of 21
Data Source
Name
Explore in Pharos
Explore in Source
Reactome
Activation of SMO
Reactome
Ca-dependent events
Reactome
CaM pathway
Reactome
Calmodulin induced events
Reactome
Cargo recognition for clathrin-mediated endocytosis
Name
Explore in Pharos
Explore in Source
Activation of SMO
Ca-dependent events
CaM pathway
Calmodulin induced events
Cargo recognition for clathrin-mediated endocytosis
Gene Ontology Terms (25)
Items per page:
10
1 – 6 of 6
GO Term
Evidence
Assigned by
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Sequence or structural Similarity (ISS)
BHF-UCL
Inferred from Sequence or structural Similarity (ISS)
BHF-UCL
Inferred from Sequence or structural Similarity (ISS)
BHF-UCL
Traceable Author Statement (TAS)
Reactome
Inferred from Electronic Annotation (IEA)
UniProtKB-KW
Protein-Protein Interactions (659)
1 – 10 of 659
GRK3
Tchem
Family: Kinase
Novelty: 0.0229797
p_int: 0.999999999
p_wrong: 1e-9
Score: 0.967
Data Source: BioPlex,STRINGDB
PPP1R16B
Tbio
Family: Enzyme
Novelty: 0.09294561
p_int: 0.999991127
p_ni: 0.000008867
p_wrong: 6e-9
Score: 0.361
Data Source: BioPlex,STRINGDB
TBC1D14
Tbio
Novelty: 0.30090271
p_int: 0.999595419
p_ni: 0.000404581
Score: 0.239
Data Source: BioPlex,STRINGDB
GNG2
Tbio
Novelty: 0.08273543
Score: 0.995
Data Source: STRINGDB
GNB1
Tbio
Novelty: 0.04716243
Score: 0.994
Data Source: STRINGDB
SMO
Tclin
Family: GPCR
Novelty: 0.04792829
Score: 0.99
Data Source: Reactome,STRINGDB
ARRB1
Tbio
Novelty: 0.00194842
Score: 0.987
Data Source: STRINGDB
ARRB2
Tbio
Novelty: 0.00180049
Score: 0.982
Data Source: STRINGDB
ADRB2
Tclin
Family: GPCR
Novelty: 0.00038334
Score: 0.981
Data Source: Reactome,STRINGDB
AGTR1
Tclin
Family: GPCR
Novelty: 0.00032594
Score: 0.98
Data Source: STRINGDB
Publication Statistics
PubMed Score  463.81

PubMed score by year
PubTator Score  470.2

PubTator score by year
Patents
Amino Acid Sequence
Residue Counts
Sequence
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRD
1-70
FCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQ
70-140
VPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRK
140-210
ADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLH
210-280
YHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHAS
280-350
VGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE
350-420
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDE
420-490
EDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKAKNKQLGHEEDYALGKDCI
490-560
MHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQF
560-630
ILQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLVQRGSANGL
630-689
MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRDFCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQVPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRKADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLHYHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHASVGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPELRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDEEDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKAKNKQLGHEEDYALGKDCIMHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQFILQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLVQRGSANGL