Property Summary

NCBI Gene PubMed Count 176
PubMed Score 411.47
PubTator Score 385.46

Knowledge Summary

Patent (12,829)

TINX Plot

  Disease Sources (3)

Disease Target Count P-value
ovarian cancer 8492 3.31472846748807E-13
osteosarcoma 7933 1.54916384219286E-10
medulloblastoma, large-cell 6234 1.27815751866589E-5
psoriasis 6685 1.87582518332629E-5
COPD 116 5.13746085565382E-4
diabetes mellitus 1663 0.00112507764568989
subependymal giant cell astrocytoma 2287 0.0499362600146897
Disease Target Count Z-score Confidence
Myocardial Infarction 126 3.256 1.6
Hypertension 293 3.251 1.6

Expression

  Differential Expression (7)

Disease log2 FC p
psoriasis 2.500 0.000
osteosarcoma 2.176 0.000
medulloblastoma, large-cell 1.200 0.000
diabetes mellitus -1.100 0.001
subependymal giant cell astrocytoma -1.209 0.050
COPD -1.300 0.001
ovarian cancer 1.400 0.000

Synonym

Accession P25098 B0ZBE1 Q13837 Q6GTT3 Beta-ARK-1
Symbols BARK1
ADRBK1
BETA-ARK1

Gene

PDB

1BAK   3CIK   3KRW   3KRX   3V5W   4MK0   4PNK   5HE1  

  Ortholog (8)

Species Source
Chimp OMA EggNOG
Macaque OMA EggNOG
Mouse OMA EggNOG Inparanoid
Rat OMA EggNOG
Cow OMA EggNOG
Pig OMA EggNOG
Anole lizard OMA EggNOG
C. elegans OMA EggNOG

MLP Assay (14)

AID Type Active / Inconclusive / Inactive Description
488806 screening 16 / 0 / 1977 RNA aptamer-based validation for inhibitors of GRK2
488847 screening 1924 / 0 / 326127 RNA aptamer-based HTS for inhibitors of GRK2
488855 summary 0 / 0 / 0 Summary Report: RNA aptamer-based HTS for inhibitors of GRK2
504451 screening 79 / 0 / 1911 Confirmation of RNA aptamer-based HTS for inhibitors of GRK2, Cherry Pick 1
504500 confirmatory 21 / 0 / 90 Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
504782 screening 8 / 0 / 354 Confirmation of RNA aptamer-based HTS for inhibitors of GRK2, Cherry Pick 2
504815 confirmatory 2 / 0 / 23 Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 2
588428 other 1 / 0 / 10 Thermofluor assay to identify compounds that bind to GRK2 and inhibit kinase activity, Set 1
588465 other 0 / 0 / 11 Kinase assay to identify compounds that inhibit phosphorylation of rhodopsin by GRK2, Set 1
588468 other 6 / 0 / 18 Thermofluor assay to identify compounds that bind to GRK2 and inhibit kinase activity, Set 2
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Gene RIF (124)

PMID Text
26706289 Acute mental stress significantly increased GRK2 density in in peripheral blood mononuclear cells of young adult males.
26670611 the dual-specific GRK2 and ERK cascade inhibitor, RKIP (Raf kinase inhibitor protein), triggered dysfunctional cardiomyocyte energetics and the expression of heart failure-promoting Pparg-regulated genes.
26447102 It plays a role in progression of Vasculature which is affected by insulin resistance and type 2 diabetes expresses high levels of GRK2
26402907 Data suggest that, by targeting/repressing GRK2, microRNA-K3 of Kaposi sarcoma-associated herpesvirus (KSHV) facilitates migration and invasion of vascular endothelial cells via activation of CXCR2/AKT signaling.
26248277 Suggest a common regulatory pattern for the beta(2)-AR/GRK2 which is independent of cellular type or pathology.
26234354 It is a critical factor in diabetic endothelial dysfunction and plays a role in many physiological functions including regulation of G-protein-coupled receptors (GPCRs). (review)
26224342 Suggest role for GRK2 in the regulating cardiac hypertrophy.
26092485 Acute aerobic exercise induces a greater GRK2 expression in women than men, while increased cardiorespiratory fitness is associated with exercise-induced GRK2 expression in PBMCs
25982117 G protein beta subunits (Gb) bind to DDB1 and Gb2 targets GRK2 for ubiquitylation by the DDB1-CUL4A-ROC1 ubiquitin ligase.
25857770 Data indicate that protein kinase GRK2 silencing abolished isoproterenol-induced phosphorylation of beta2-adrenergic receptor (beta2ARs).
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AA Sequence

MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRD      1 - 70
FCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQ     71 - 140
VPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRK    141 - 210
ADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLH    211 - 280
YHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHAS    281 - 350
VGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE    351 - 420
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDE    421 - 490
EDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKAKNKQLGHEEDYALGKDCI    491 - 560
MHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQF    561 - 630
ILQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLVQRGSANGL               631 - 689
//

Text Mined References (180)

PMID Year Title
26706289 2016 G protein-coupled receptor kinase-2 in peripheral blood mononuclear cells following acute mental stress.
26670611 2016 Inhibition of G-protein-coupled Receptor Kinase 2 Prevents the Dysfunctional Cardiac Substrate Metabolism in Fatty Acid Synthase Transgenic Mice.
26447102 2015 G-protein-coupled receptor kinase 2 and endothelial dysfunction: molecular insights and pathophysiological mechanisms.
26402907 2015 A KSHV microRNA Directly Targets G Protein-Coupled Receptor Kinase 2 to Promote the Migration and Invasion of Endothelial Cells by Inducing CXCR2 and Activating AKT Signaling.
26248277 2015 ?2- and ?1-Adrenoceptor Expression Exhibits a Common Regulatory Pattern With GRK2 and GRK5 in Human and Animal Models of Cardiovascular Diseases.
26234354 2015 [The Role of GRK2 and Its Potential as a New Therapeutic Target in Diabetic Vascular Complications].
26224342 2015 Integrating GRK2 and NFkappaB in the Pathophysiology of Cardiac Hypertrophy.
26092485 2015 Acute aerobic exercise mediates G protein-coupled receptor kinase 2 expression in human PBMCs.
25982117 2015 A Non-Canonical Function of G? as a Subunit of E3 Ligase in Targeting GRK2 Ubiquitylation.
25857770 2015 Membrane-permeable tastants amplify ?2-adrenergic receptor signaling and delay receptor desensitization via intracellular inhibition of GRK2's kinase activity.
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