Affinage

GRK3

G protein-coupled receptor kinase 3 · UniProt P35626

Length
688 aa
Mass
79.7 kDa
Annotated
2026-04-28
40 papers in source corpus 26 papers cited in narrative 26 extracted findings

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

GRK3 is a G protein-coupled receptor kinase that phosphorylates agonist-activated GPCRs to initiate β-arrestin recruitment, receptor desensitization, and internalization across diverse receptor systems including odorant, opioid, adrenergic, CRF1, CXCR4, and platelet GPCRs (PMID:9325250, PMID:18274673, PMID:39419098). Beyond its kinase-dependent role, GRK3 inhibits Gq signaling through its RGS homology (RH) domain independently of catalytic activity, as demonstrated by suppression of L-DOPA-induced dyskinesia in a parkinsonian model (PMID:26043205). GRK3 also phosphorylates the non-GPCR substrate HDAC2 at serine 394, enhancing epigenetic repression of tumor suppressors to promote angiogenesis and neuroendocrine differentiation in prostate cancer (PMID:37543278). Selective membrane recruitment of GRK3 is governed by Gβ5-containing Gβγ dimers, distinguishing it from the closely related GRK2 (PMID:39579957).

Mechanistic history

Synthesis pass · year-by-year structured walk · 13 steps
  1. 1997 High

    Establishing that GRK3 is a physiologically essential GPCR kinase for sensory receptor desensitization resolved whether GRK2 and GRK3 had redundant functions in vivo.

    Evidence GRK3 knockout mice showed abolished fast odorant-induced desensitization and reduced cAMP generation in olfactory cilia

    PMID:9325250

    Open questions at the time
    • Whether GRK3 phosphorylation sites on odorant receptors were mapped
    • Whether GRK2 can partially compensate in olfactory neurons over longer timescales
  2. 1998 High

    Demonstrating cardiac substrate selectivity of GRK3 established that GRK isoforms have non-overlapping receptor preferences even within the same tissue.

    Evidence Transgenic cardiac GRK3 overexpression attenuated thrombin-induced MAPK signaling but not β-adrenergic or angiotensin II receptor responses in mouse heart

    PMID:9746479

    Open questions at the time
    • Identity of the thrombin receptor (PAR) phosphorylation sites targeted by GRK3
    • Whether endogenous GRK3 levels limit thrombin signaling under physiological conditions
  3. 2001 Medium

    Identifying GRK3 as the kinase mediating CRF1 receptor desensitization extended its substrate repertoire to stress-related neuropeptide receptors.

    Evidence GRK3 antisense knockdown inhibited CRF1 desensitization by ~65% in Y-79 cells while PKA inhibition had no effect

    PMID:11247813

    Open questions at the time
    • Awaits confirmation by genetic knockout or CRISPR approaches
    • CRF1 phosphorylation sites targeted by GRK3 not mapped
  4. 2003 High

    Showing that GRK3 is required for tolerance to high-efficacy but not low-efficacy opioids revealed an agonist-efficacy threshold for GRK3-dependent desensitization, a principle later extended to MOR-ERK signaling.

    Evidence GRK3 knockout mice retained morphine tolerance but lost fentanyl tolerance in hippocampal electrophysiology and antinociception assays

    PMID:14662727

    Open questions at the time
    • Whether GRK3 directly phosphorylates KOR/MOR or acts indirectly
    • Relative contributions of GRK2 vs GRK3 to opioid tolerance
  5. 2006 High

    Demonstrating that GRK3 phosphorylation of KOR-Ser369 enables arrestin3-dependent p38 MAPK activation, and that GRK3-arrestin3 mediates MOR-ERK1/2 signaling, established GRK3 as a signaling scaffold beyond simple desensitization.

    Evidence GRK3 KO neurons lacked KOR-p38 and MOR-ERK activation; dominant-positive arrestin3-R170E rescued signaling; KOR-S369A mutant was refractory

    PMID:16648139 PMID:16982618

    Open questions at the time
    • Structural basis of GRK3 selectivity for Ser369 on KOR
    • Whether GRK3-arrestin scaffolding occurs for non-opioid GPCRs
  6. 2007 High

    Identifying GRK3 as a specific desensitizer of cardiac α1-adrenergic receptors with blood pressure consequences defined a non-redundant cardiovascular role for GRK3 distinct from GRK2.

    Evidence Transgenic expression of dominant-negative GRK3ct enhanced α1-AR ERK signaling in myocytes and raised systolic blood pressure in mice

    PMID:18165681

    Open questions at the time
    • Direct identification of α1-AR phosphorylation sites by GRK3
    • Whether GRK3 contributes to hypertension in human disease
  7. 2008 High

    Showing that GRK3 silencing phenocopied WHIM syndrome CXCR4 dysfunction — and GRK3 overexpression rescued it — identified GRK3 as the physiological kinase for CXCR4 desensitization in leukocytes.

    Evidence GRK3 siRNA in control leukocytes impaired CXCR4 internalization and chemotaxis; GRK3 overexpression in WHIM patient cells restored both

    PMID:18274673

    Open questions at the time
    • CXCR4 phosphorylation sites preferentially targeted by GRK3 vs GRK2
    • Whether GRK3 variants contribute to WHIM-like phenotypes
  8. 2009 High

    Engineering the GRK3 C-terminal Gβγ-binding domain as a biosensor proved that this domain selectively recognizes free Gβγ, confirming a structural basis for GRK3 membrane recruitment.

    Evidence FRET/BRET with GRK3ct-fluorescent fusions showed binding to free Gβγ but not intact heterotrimers, resolving G protein dissociation kinetics (<100 ms)

    PMID:19258039

    Open questions at the time
    • Whether endogenous GRK3 recruitment follows the same kinetics
    • Structural details of GRK3ct-Gβγ interface
  9. 2015 High

    Dissecting the RH domain function of GRK3 revealed a kinase-independent Gq-inhibitory mechanism, expanding GRK3's functional repertoire beyond phosphorylation.

    Evidence Kinase-dead GRK3 retained suppression of L-DOPA dyskinesia in hemiparkinsonian rats, but RH-domain-disabled GRK3 did not; RH domain bound striatal Gq directly

    PMID:26043205

    Open questions at the time
    • Structural basis of RH domain-Gq interaction
    • Whether the RH domain contributes to GRK3 function at other Gq-coupled receptors
  10. 2020 High

    CRISPR dissection of GRK2/3 contributions to MOR internalization showed both kinases contribute with GRK2 dominant, and revealed a GRK2/3-independent β-arrestin2 recruitment component.

    Evidence CRISPR KO of GRK2, GRK3, or both in HEK293 cells with rescue; BRET β-arrestin2 recruitment and flow cytometry internalization across multiple agonists

    PMID:33060647

    Open questions at the time
    • Phosphosite-level comparison of GRK2 vs GRK3 on MOR
    • Identity of the GRK-independent β-arrestin recruitment mechanism
  11. 2023 Medium

    Discovery that GRK3 phosphorylates the non-GPCR substrate HDAC2 at Ser394 to enhance epigenetic repression established a kinase-dependent oncogenic mechanism distinct from GPCR desensitization.

    Evidence Co-IP, in vitro phosphorylation, ChIP showing HDAC2 enrichment at TSP1/REST promoters, and xenograft models in prostate cancer

    PMID:37543278

    Open questions at the time
    • Whether GRK3-HDAC2 interaction occurs outside prostate cancer contexts
    • Full phosphoproteomics of non-GPCR GRK3 substrates not performed
  12. 2024 High

    Identification of Gβ5 as a selective determinant distinguishing GRK3 from GRK2 membrane recruitment resolved a long-standing question about how two highly homologous kinases achieve substrate selectivity.

    Evidence CRISPR KO of Gβ subunits, single-molecule imaging of GRK3 at confined membrane domains enriched in Gβ5, BRET/FRET assays with biased MOR agonists

    PMID:39579957

    Open questions at the time
    • Structural basis for Gβ5 selectivity toward GRK3 over GRK2
    • Whether Gβ5-GRK3 selectivity generalizes to all GPCR substrates
  13. 2024 High

    Demonstrating that GRK3 loss potentiates platelet GPCR signaling across Gq-, Gi-, and Gz-coupled receptors defined GRK3 as a broad platelet GPCR desensitizer relevant to hemostasis.

    Evidence GRK3 KO mouse platelets showed enhanced aggregation and secretion to multiple GPCR agonists but not collagen; shorter tail bleeding times in vivo

    PMID:39419098

    Open questions at the time
    • Specific platelet GPCR phosphorylation sites targeted by GRK3
    • Whether GRK3 variants affect bleeding or thrombotic risk in humans

Open questions

Synthesis pass · forward-looking unresolved questions
  • The full spectrum of non-GPCR substrates of GRK3, the structural basis for Gβ5-mediated selective membrane recruitment, and whether GRK3 kinase vs RH domain functions are coordinately regulated remain unresolved.
  • No unbiased phosphoproteomics for GRK3 substrates
  • No high-resolution structure of GRK3 in complex with Gβ5 or Gq
  • Coordinate regulation of kinase and RH domain activities not addressed

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0140096 catalytic activity, acting on a protein 8 GO:0008289 lipid binding 2 GO:0098772 molecular function regulator activity 1
Localization
GO:0005886 plasma membrane 3 GO:0005829 cytosol 2
Pathway
R-HSA-162582 Signal Transduction 11 R-HSA-1643685 Disease 3 R-HSA-168256 Immune System 2 R-HSA-109582 Hemostasis 1
Partners
ARRB2CXCR4GNAQGNB5HDAC2OPRK1OPRM1RKIP

Evidence

Reading pass · 26 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
1997 GRK3 is required for agonist-induced desensitization of odorant receptors in the olfactory epithelium; GRK3 knockout mice lack fast agonist-induced desensitization and show markedly reduced cAMP generation following odorant stimulation. GRK3 knockout mice, cilia preparation cAMP assay, odorant stimulation The Journal of biological chemistry High 9325250
1998 Cardiac overexpression of GRK3 selectively attenuates thrombin-induced p42/p44 MAP kinase activation but does not desensitize beta-adrenergic or angiotensin II receptors in vivo, demonstrating distinct substrate specificity of GRK3 in the heart. Transgenic mice with cardiac-specific GRK3 overexpression, in vivo hemodynamic measurements, MAP kinase activation assays The American journal of physiology High 9746479
2001 GRK3 mediates homologous desensitization of CRF1 receptors; GRK3 antisense knockdown (~50% reduction in GRK3 protein) inhibited CRF1 receptor desensitization by ~65% in Y-79 cells, while PKA inhibition had no effect. GRK3 antisense oligonucleotide and antisense cDNA transfection, cAMP accumulation assay, heparin GRK inhibition American journal of physiology. Regulatory, integrative and comparative physiology Medium 11247813
2003 GRK3-mediated mechanisms are required for electrophysiological and behavioral tolerance to the high-efficacy opioid fentanyl but not morphine; GRK3 knockout mice show significantly reduced fentanyl tolerance in hippocampal slices and antinociceptive assays. GRK3 knockout mice, hippocampal slice electrophysiology, hot-plate antinociception assay British journal of pharmacology High 14662727
2003 Beta2-adrenoceptor activation upregulates GRK3 expression, which in turn mediates desensitization and downregulation of alpha2A-adrenoceptors; GRK2/3 antisense DNA blocked chronic adrenaline-induced alpha2A-AR desensitization. GRK2/3 antisense DNA, receptor binding assay, beta-AR antagonist propranolol blockade, immunoblotting British journal of pharmacology Medium 12642394
2005 ATP stimulates GRK3 binding to the P2X7 receptor, followed by beta-arrestin-2 and dynamin recruitment, leading to clathrin-dependent internalization of the receptor. Western blot co-immunoprecipitation, pore formation assay, immunofluorescence of beta-arrestin-2 redistribution American journal of physiology. Cell physiology Medium 15728711
2006 KOR activation of p38 MAPK requires GRK3-mediated phosphorylation of serine-369 on KOR and subsequent arrestin3 recruitment; p38 activation was absent in GRK3 knockout neurons and astrocytes, and was rescued by dominant-positive arrestin3-(R170E). GRK3 knockout mice, AtT-20 cells with KSA mutant receptor, dominant-positive arrestin3-(R170E) transfection, phospho-p38 immunolabeling, siRNA for arrestin3 The Journal of biological chemistry High 16648139
2006 Mu opioid receptor activation of ERK1/2 in striatal neurons requires GRK3 and arrestin3; ERK1/2 activation by fentanyl was absent in GRK3-/- neurons and restored by dominant-positive arrestin3-(R170E), and was not induced by morphine (lower efficacy) unless dominant-positive arrestin was co-expressed. GRK3 knockout mice, MOR knockout mice, dominant-positive arrestin3-(R170E) transfection, siRNA for arrestin3, MEK inhibitor U0126, ERK1/2 phosphorylation assay The Journal of biological chemistry High 16982618
2006 Chronic treatment with lithium or carbamazepine (but not valproate) increases translocation of GRK3 from cytosol to membrane fraction in rat frontal cortex. Immunoblotting of membrane and cytosol fractions from drug-treated rats Biological psychiatry Low 16697355
2007 CRF activates CRF1 receptors to upregulate GRK3 expression via an ERK1/2-mediated mechanism involving Sp-1 and Ap-2 transcription factors in CATH.a cells (locus coeruleus-derived). ERK1/2 inhibitors, transcription factor activity assays (Sp-1, Ap-2), GRK3 mRNA/protein quantification FEBS letters Medium 17583697
2007 Inhibition of cardiac GRK3 (via expression of GRK3ct) enhances alpha1-adrenergic receptor-mediated ERK1/2 activation in cardiac myocytes and increases systolic blood pressure and cardiac output in vivo, demonstrating that GRK3 specifically desensitizes alpha1-adrenergic receptors in the heart. Transgenic mice expressing GRK3ct competitive inhibitor, cardiac myocyte ERK1/2 assay, conductance micromanometry, tail-cuff plethysmography, radiotelemetric blood pressure recording The Journal of biological chemistry High 18165681
2008 GRK3 specifically regulates CXCL12-promoted internalization and desensitization of CXCR4; GRK3 silencing in control leukocytes phenocopied impaired CXCR4 attenuation seen in WHIM syndrome cells, and GRK3 overexpression in WHIM patient cells restored normal CXCR4 internalization and chemotaxis. GRK3 siRNA knockdown, GRK3 overexpression in patient leukocytes and fibroblasts, CXCR4 internalization assay, chemotaxis assay The Journal of clinical investigation High 18274673
2009 The C-terminus of GRK3 (GRK3ct) fused to fluorescent reporters binds free Gbetagamma dimers but not intact heterotrimers, enabling real-time reporting of G protein heterotrimer dissociation; using this probe, heterotrimer dissociation in living cells was shown to occur in less than 100 ms. FRET/BRET with GRK3ct fusion proteins and venus-labeled Gbetagamma, live-cell imaging, kinetic analysis Cellular signalling High 19258039
2014 GRK3 promotes prostate cancer metastasis and angiogenesis, at least in part through downregulation of thrombospondin-1 and plasminogen activator inhibitor type 2; GRK3 is necessary for survival/proliferation of metastatic cells and sufficient to promote primary tumor growth in mouse xenograft models. RNAi screen, cDNA overexpression screen, mouse xenograft models, angiogenesis assays, protein expression analysis Proceedings of the National Academy of Sciences of the United States of America Medium 24434559
2015 GRK3 suppresses L-DOPA-induced dyskinesia via its RGS homology (RH) domain, which binds striatal Gq; kinase-dead GRK3 retains suppressive activity, but GRK3 with disabled RH domain does not, indicating the RH domain mediates Gq inhibition independently of kinase activity. Viral vector-mediated overexpression and microRNA knockdown in hemiparkinsonian rats, domain mutant analysis, Gq binding assay, ΔFosB immunohistochemistry Scientific reports High 26043205
2016 CREB directly targets and induces GRK3 transcription; GRK3 promotes neuroendocrine differentiation of prostate cancer cells in a kinase activity-dependent manner, and GRK3 silencing blocks CREB-induced neuroendocrine differentiation. ChIP/promoter analysis for CREB binding, GRK3 overexpression with kinase-dead controls, siRNA knockdown, NE marker expression assays Oncotarget Medium 27191986
2019 RKIP binds specifically to the N-termini of GRK2 and GRK3 (not GRK5); the isolated N-terminal domains (GRK2/3 residues 1-185) interact directly with beta2-AR, prevent its phosphorylation and internalization, and increase receptor signaling and cardiomyocyte contractility. Co-immunoprecipitation, pull-down assays, beta2-AR phosphorylation assay, receptor internalization assay, cardiomyocyte contractility measurement Biochemical and biophysical research communications Medium 31604529
2020 GRK3 is recruited to chemokine-stimulated ACKR4 prior to beta-arrestins, and GRK2/3 inhibition partially blocks steady-state and chemokine-driven beta-arrestin recruitment to ACKR4, placing GRK3 upstream of beta-arrestin in ACKR4 trafficking. BRET-based GRK and beta-arrestin recruitment assays, GRK2/3 pharmacological inhibition, ACKR4 C-terminus deletion, fluorescent chemokine uptake assay Frontiers in immunology Medium 32391018
2020 GRK2 and GRK3 are both required for mu-opioid receptor internalization and beta-arrestin2 recruitment; GRK2 contributes more than GRK3, and a GRK2/3-independent component of beta-arrestin2 recruitment exists at the plasma membrane. CRISPR/Cas9 knockout of GRK2, GRK3, or both in HEK293 cells; rescue expression; CMPD101 pharmacological inhibition; BRET-based beta-arrestin2 recruitment; flow cytometry internalization assay Scientific reports High 33060647
2021 GRK3 deficiency in mice leads to elevated brain IL-1β, increased kynurenic acid turnover, hyper-responsiveness to D-amphetamine, elevated spontaneous firing of midbrain dopamine neurons, and disruption in prepulse inhibition, linking GRK3 to immune/glial activation and dopaminergic dysregulation. Grk3-/- mice, behavioral assays, electrophysiology, biochemical (IL-1β, KYNA measurements), molecular imaging Molecular psychiatry Medium 33976392
2023 GRK3 phosphorylates HDAC2 at serine 394, enhancing HDAC2's epigenetic repression of TSP1 and REST, thereby promoting angiogenesis and neuroendocrine differentiation in prostate cancer. Co-IP, phosphorylation assay (GRK3-HDAC2 at S394), ChIP, luciferase reporter assay, siRNA/overexpression, in vivo xenograft Cancer letters Medium 37543278
2023 GRK3 deficiency enhances osteoclastogenesis and proliferation of hematopoietic osteoclast precursors in vitro and in vivo; aged Grk3-/- mice develop bone lesions resembling Paget's Disease of Bone. Grk3-/- mice, in vitro osteoclast differentiation assay, flow cytometry of hematopoietic precursors, histological analysis Cells Medium 37048054
2024 GRK3 plays a distinct role in platelet GPCR desensitization: GRK3-/- platelets show potentiated aggregation and secretion in response to multiple GPCR agonists (including Gq-, Gi-, and Gz-coupled receptors) but not to the non-GPCR agonist collagen; GRK3-/- mice show shorter tail bleeding times. GRK3 knockout mice, platelet aggregation assay, dense granule secretion assay, AKT and ERK phosphorylation, tail bleeding time Thrombosis and haemostasis High 39419098
2024 Gβ5 selectively distinguishes GRK3 from GRK2 and enables GRK3 recruitment to the plasma membrane upon MOR activation; GRK3 is recruited to confined membrane domains enriched in Gβ5 (via single-molecule imaging), and oliceridine (a G-protein-biased MOR agonist) selectively activates GRK3-mediated beta-arrestin recruitment via Gαz-Gβ5 signaling. Multiple CRISPR-edited cell lines, BRET/FRET functional assays, single-molecule imaging, particle diffusion analysis European journal of pharmacology High 39579957
2007 GRK3 regulates GRK2 protein levels in U937 cells via a mechanism involving inositol phosphate (InsP) upregulation; GRK3 antisense knockdown decreased GRK2 levels, establishing a novel cross-regulatory mechanism between GRK family members. Antisense knockdown of GRK3, immunoblotting for GRK2, InsP measurement Biochemical pharmacology Low 17433264
2025 GRK2, GRK3, and GRK6 are all important for FPR1 internalization in neutrophil-like cells, as identified by genome-wide CRISPR/Cas9 screens; FPR1 uses multiple endocytic pathways since cells lacking beta-arrestins show strong but incomplete internalization defects. Genome-wide CRISPR/Cas9 screens, FPR1 surface expression and internalization assays, beta-arrestin knockout validation bioRxivpreprint Medium bio_10.1101_2025.04.21.649864

Source papers

Stage 0 corpus · 40 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2006 Kappa opioid receptor activation of p38 MAPK is GRK3- and arrestin-dependent in neurons and astrocytes. The Journal of biological chemistry 203 16648139
2009 The c-terminus of GRK3 indicates rapid dissociation of G protein heterotrimers. Cellular signalling 147 19258039
1997 G protein-coupled receptor kinase 3 (GRK3) gene disruption leads to loss of odorant receptor desensitization. The Journal of biological chemistry 129 9325250
2008 Leukocyte analysis from WHIM syndrome patients reveals a pivotal role for GRK3 in CXCR4 signaling. The Journal of clinical investigation 109 18274673
2003 G-protein receptor kinase 3 (GRK3) influences opioid analgesic tolerance but not opioid withdrawal. British journal of pharmacology 85 14662727
2006 Mu opioid receptor activation of ERK1/2 is GRK3 and arrestin dependent in striatal neurons. The Journal of biological chemistry 65 16982618
2005 ATP stimulates GRK-3 phosphorylation and beta-arrestin-2-dependent internalization of P2X7 receptor. American journal of physiology. Cell physiology 59 15728711
1998 Myocardial overexpression of GRK3 in transgenic mice: evidence for in vivo selectivity of GRKs. The American journal of physiology 52 9746479
2020 ACKR4 Recruits GRK3 Prior to β-Arrestins but Can Scavenge Chemokines in the Absence of β-Arrestins. Frontiers in immunology 45 32391018
2001 GRK3 mediates desensitization of CRF1 receptors: a potential mechanism regulating stress adaptation. American journal of physiology. Regulatory, integrative and comparative physiology 45 11247813
2020 Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells. Scientific reports 44 33060647
2016 GRK3 is a direct target of CREB activation and regulates neuroendocrine differentiation of prostate cancer cells. Oncotarget 41 27191986
1994 Chromosome mapping of the human arrestin (SAG), beta-arrestin 2 (ARRB2), and beta-adrenergic receptor kinase 2 (ADRBK2) genes. Genomics 41 7695743
2014 GRK3 is essential for metastatic cells and promotes prostate tumor progression. Proceedings of the National Academy of Sciences of the United States of America 37 24434559
2002 GRK3 regulation during CRF- and urocortin-induced CRF1 receptor desensitization. Biochemical and biophysical research communications 35 12413940
2007 Cardiac-restricted expression of the carboxyl-terminal fragment of GRK3 Uncovers Distinct Functions of GRK3 in regulation of cardiac contractility and growth: GRK3 controls cardiac alpha1-adrenergic receptor responsiveness. The Journal of biological chemistry 30 18165681
2010 beta-Adrenoceptor and GRK3 expression in human lymphocytes is related to blood pressure and urinary albumin excretion. Journal of hypertension 24 20216086
2011 Differential effects of inescapable stress on locus coeruleus GRK3, alpha2-adrenoceptor and CRF1 receptor levels in learned helpless and non-helpless rats: a potential link to stress resilience. Behavioural brain research 23 21333691
2006 Chronic treatment with mood stabilizers increases membrane GRK3 in rat frontal cortex. Biological psychiatry 20 16697355
2015 GRK3 suppresses L-DOPA-induced dyskinesia in the rat model of Parkinson's disease via its RGS homology domain. Scientific reports 17 26043205
2007 Further evidence for association of GRK3 to bipolar disorder suggests a second disease mutation. Psychiatric genetics 17 18075471
2003 Desensitization of alpha 2A-adrenoceptor signalling by modest levels of adrenaline is facilitated by beta 2-adrenoceptor-dependent GRK3 up-regulation. British journal of pharmacology 17 12642394
2019 Pharmacological antagonism of histamine H2R ameliorated L-DOPA-induced dyskinesia via normalization of GRK3 and by suppressing FosB and ERK in PD. Neurobiology of aging 16 31306812
2009 Decreased GRK3 but not GRK2 expression in frontal cortex from bipolar disorder patients. The international journal of neuropsychopharmacology 13 19400979
2007 Activation of the CRF(1) receptor causes ERK1/2 mediated increase in GRK3 expression in CATH.a cells. FEBS letters 12 17583697
2006 Bipolar 1 disorder is not associated with the RGS4, PRODH, COMT and GRK3 genes. Psychiatric genetics 12 17106420
2021 GRK3 deficiency elicits brain immune activation and psychosis. Molecular psychiatry 11 33976392
2011 Activity of β2-adrenergic receptor in oral squamous cell carcinoma is mediated by overexpression of the ADRBK2 gene: a pilot study. Biotechnic & histochemistry : official publication of the Biological Stain Commission 10 21916780
2023 A novel GRK3-HDAC2 regulatory pathway is a key direct link between neuroendocrine differentiation and angiogenesis in prostate cancer progression. Cancer letters 9 37543278
2019 The N-termini of GRK2 and GRK3 simulate the stimulating effects of RKIP on β-adrenoceptors. Biochemical and biophysical research communications 8 31604529
2009 Allele specific analysis of the ADRBK2 gene in lymphoblastoid cells from bipolar disorder patients. Journal of psychiatric research 8 19766236
2005 Lymphocyte G-protein receptor kinase (GRK)3 mRNA levels in bipolar disorder. The international journal of neuropsychopharmacology 8 16359584
2023 TEAD3 inhibits the proliferation and metastasis of prostate cancer via suppressing ADRBK2. Biochemical and biophysical research communications 6 36907139
2007 Association analysis of GRK3 gene promoter variants in cocaine abuse. Psychiatric genetics 5 17621168
2024 TRIM58 downregulation maintains stemness via MYH9-GRK3-YAP axis activation in triple-negative breast cancer stem cells. Cancer gene therapy 4 38714850
2024 Signal profiles and spatial regulation of β-arrestin recruitment through Gβ5 and GRK3 at the μ-opioid receptor. European journal of pharmacology 2 39579957
2023 Aged G Protein-Coupled Receptor Kinase 3 (Grk3)-Deficient Mice Exhibit Enhanced Osteoclastogenesis and Develop Bone Lesions Analogous to Human Paget's Disease of Bone. Cells 1 37048054
2024 Distinct Role of GRK3 in Platelet Activation by Desensitization of G Protein-Coupled Receptors. Thrombosis and haemostasis 0 39419098
2018 G Protein-Coupled Receptor Kinase 3 (GRK3) in Olfaction. Methods in molecular biology (Clifton, N.J.) 0 29884935
2007 Regulatory mechanisms underlying GKR2 levels in U937 cells: evidence for GRK3 involvement. Biochemical pharmacology 0 17433264