Property Summary

NCBI Gene PubMed Count 176
Grant Count 329
R01 Count 207
Funding $40,748,837.47
PubMed Score 411.47
PubTator Score 385.46

Knowledge Summary

Patent (12,829)

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  

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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