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Grk2 - G protein-coupled receptor kinase 2 Gene

Also Known as BARK1; GRK-2; Adrbk1

Species: Rattus norvegicus

Gene Type: protein coding

Gene ID: 25238

Summary

Enables several functions, including Opioid Receptor binding activity; protein kinase activity; and scaffold protein binding activity. Involved in several processes, including blood vessel diameter maintenance; negative regulation of G protein-coupled receptor signaling pathway; and negative regulation of cellular protein metabolic process. Located in several cellular components, including basolateral plasma membrane; caveola; and dendrite. Used to study hyperglycemia; impotence; and limb ischemia. Biomarker of Parkinson's disease; congestive heart failure; hypertension; and portal hypertension. Orthologous to human GRK2 (G protein-coupled receptor kinase 2). [provided by Alliance of Genome Resources, Apr 2022]

Grk2 Products (1)

mRNA	Protein	Name
NM_012776.2	NP_036908.2	beta-adrenergic receptor kinase 1

Gene Ontology

Molecular Function
Biological Process
Cellular Component

Molecular Function GO Annotation	Evidence	References	Source
enables G protein-coupled receptor binding	IPI IPI: Inferred from physical interaction	26228571	RGD
enables G protein-coupled receptor kinase activity	IDA IDA: Inferred from direct assay	1403099	RGD
enables beta-adrenergic receptor kinase activity	IDA IDA: Inferred from direct assay	1403099	RGD
enables delta-type opioid receptor binding	IPI IPI: Inferred from physical interaction	28381559	RGD
enables kappa-type opioid receptor binding	IPI IPI: Inferred from physical interaction	27865836	RGD
enables protein binding	IPI IPI: Inferred from physical interaction	15626685	RGD
enables scaffold protein binding	IPI IPI: Inferred from physical interaction	28162981	RGD
enables ubiquitin protein ligase binding	IPI IPI: Inferred from physical interaction	26228571	RGD

Biological Process GO Annotation	Evidence	References	Source
involved in G protein-coupled receptor signaling pathway	IDA IDA: Inferred from direct assay	12021252	RGD
involved in G protein-coupled receptor signaling pathway	IEP IEP: Inferred from expression pattern	29081032	RGD
involved in cellular response to catecholamine stimulus	IEP IEP: Inferred from expression pattern	26849467	RGD
involved in cellular response to chemokine	IDA IDA: Inferred from direct assay	23221335	RGD
involved in cellular response to epidermal growth factor stimulus	IMP IMP: Inferred from mutant phenotype	24018045	RGD
involved in cellular response to glucose stimulus	IDA IDA: Inferred from direct assay	27865836	RGD
involved in cellular response to organic cyclic compound	IEP IEP: Inferred from expression pattern	23467820	RGD
involved in cellular response to phorbol 13-acetate 12-myristate	IEP IEP: Inferred from expression pattern	29905975	RGD
involved in cellular response to rapamycin	IEP IEP: Inferred from expression pattern	26228571	RGD
involved in desensitization of G protein-coupled receptor signaling pathway	IDA IDA: Inferred from direct assay	18223549	RGD
involved in desensitization of G protein-coupled receptor signaling pathway	IMP IMP: Inferred from mutant phenotype	17908240	RGD
involved in follicle-stimulating hormone signaling pathway	IDA IDA: Inferred from direct assay	16899567	RGD
involved in maintenance of protein location in nucleus	IMP IMP: Inferred from mutant phenotype	28759639	RGD
involved in negative regulation of D-glucose import	IMP IMP: Inferred from mutant phenotype	26660861	RGD
involved in negative regulation of G protein-coupled receptor signaling pathway	IDA IDA: Inferred from direct assay	1403099	RGD
involved in negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway	IMP IMP: Inferred from mutant phenotype	30075183	RGD
involved in negative regulation of apoptotic process	IMP IMP: Inferred from mutant phenotype	26849467	RGD
involved in negative regulation of cellular response to insulin stimulus	IMP IMP: Inferred from mutant phenotype	23913704	RGD
involved in negative regulation of cysteine-type endopeptidase activity	IMP IMP: Inferred from mutant phenotype	23690069	RGD
involved in negative regulation of peptidyl-serine phosphorylation	IMP IMP: Inferred from mutant phenotype	26660861	RGD
involved in negative regulation of peptidyl-threonine phosphorylation	IMP IMP: Inferred from mutant phenotype	26660861	RGD
involved in oligodendrocyte differentiation	IEP IEP: Inferred from expression pattern	24613411	RGD
involved in oligodendrocyte differentiation	IMP IMP: Inferred from mutant phenotype	24613411	RGD
involved in positive regulation of catecholamine secretion	IDA IDA: Inferred from direct assay	18223549	RGD
involved in positive regulation of excitatory postsynaptic potential	IMP IMP: Inferred from mutant phenotype	28975565	RGD
involved in positive regulation of fibroblast proliferation	IMP IMP: Inferred from mutant phenotype	27862165	RGD
involved in positive regulation of interleukin-6 production	IMP IMP: Inferred from mutant phenotype	28193640	RGD
involved in positive regulation of muscle cell apoptotic process	IMP IMP: Inferred from mutant phenotype	26631573	RGD
involved in positive regulation of vascular associated smooth muscle cell proliferation	IMP IMP: Inferred from mutant phenotype	24018045	RGD
involved in positive regulation of vasoconstriction	IMP IMP: Inferred from mutant phenotype	28882814	RGD
involved in protein phosphorylation	IDA IDA: Inferred from direct assay	1403099	RGD
involved in protein phosphorylation	IMP IMP: Inferred from mutant phenotype	23690069	RGD
involved in regulation of inositol trisphosphate biosynthetic process	IMP IMP: Inferred from mutant phenotype	20705669	RGD
involved in response to caloric restriction	IEP IEP: Inferred from expression pattern	23073237	RGD
involved in response to hydrogen peroxide	IEP IEP: Inferred from expression pattern	16337875	RGD
involved in response to leptin	IEP IEP: Inferred from expression pattern	23073237	RGD
involved in response to muscle activity	IEP IEP: Inferred from expression pattern	23913704	RGD
involved in response to organic cyclic compound	IDA IDA: Inferred from direct assay	16478977	RGD
involved in response to oxidative stress	IDA IDA: Inferred from direct assay	16478977	RGD
involved in vasodilation	IMP IMP: Inferred from mutant phenotype	23913704	RGD

Cellular Component GO Annotation	Evidence	References	Source
located in apical plasma membrane	IDA IDA: Inferred from direct assay	16899567	RGD
located in axon	IDA IDA: Inferred from direct assay	1403099	RGD
located in basolateral plasma membrane	IDA IDA: Inferred from direct assay	16899567	RGD
located in caveola	IDA IDA: Inferred from direct assay	15626685	RGD
located in dendritic shaft	IDA IDA: Inferred from direct assay	1403099	RGD
located in dendritic spine	IDA IDA: Inferred from direct assay	1403099	RGD
is active in glutamatergic synapse	IDA IDA: Inferred from direct assay	1403099	RGD
is active in postsynaptic density	IDA IDA: Inferred from direct assay	1403099	RGD
is active in presynapse	IDA IDA: Inferred from direct assay	1403099	RGD

EXP: Inferred from Experiment IDA: Inferred from direct assay IPI: Inferred from physical interaction IMP: Inferred from mutant phenotype IGI: Inferred from genetic interaction IEP: Inferred from expression pattern

Protein Preferred Names	Protein Names
beta-adrenergic receptor kinase 1	adrenergic receptor kinase, beta 1 adrenergic, beta, receptor kinase 1 beta-ARK-1 beta-adrenergic receptor kinase 1 beta ARK1

Related Agents

Approval
Pre-clinical Phase

Approval

Bioactive Molecules (1)

Cat. No.	Product Name	Effect	Purity	Rare Diseases
HY-B0492A	Paroxetine hydrochloride hemihydrate	Inhibitor	99.96%	Unkown

Pre-clinical Phase

Bioactive Molecules (32)

Cat. No.	Product Name	Effect	Purity	Rare Diseases
HY-103045	CMPD101	Inhibitor	99.49%	Unkown
HY-18991	CCG215022	Inhibitor	99.79%	Unkown
HY-109562A	CCG258208 hydrochloride		98.05%	Unkown
HY-121983	CAY10594	Modulator	98.64%	Unkown
HY-156863	GRK2 Inhibitor 2	Inhibitor	99.92%	Unkown
HY-W013411A	Locostatin	Inhibitor	99.88%	Unkown
HY-18990	GSK180736A	Inhibitor	98.81%	Unkown
HY-47573	CCG273441	Inhibitor	98.78%	Unkown
HY-123538	GRK2 Inhibitor 1	Inhibitor	98.06%	Unkown
HY-139690	CCG258747	Inhibitor	98.96%	Unkown
HY-P1396A	GRK2i TFA	Inhibitor	99.89%	Unkown
HY-177948	GRK2 degrader-1	Degrader	98.83%	Unkown
HY-RS05813	GRK2 Human Pre-designed siRNA Set A	Inhibitor	/	Unkown
HY-129118	Takeda103A	Inhibitor	98.69%	Unkown
HY-109562	CCG258208	Inhibitor	/	Unkown
HY-183057	GRK2 modulator 1	Modulator	/	Unkown
HY-179707	GRL-03022	Inhibitor	/	Unkown
HY-150022	GRK5-IN-4	Inhibitor	/	Unkown
HY-150039	CCG-271423	Inhibitor	/	Unkown
HY-P1396	GRK2i	Inhibitor	/	Unkown
HY-103045A	CMPD101 hydrochloride	Inhibitor	/	Unkown
HY-155099	FGH31		/	Unkown
HY-120168	CCG 258001	Inhibitor	/	Unkown
HY-B0492S1	Paroxetine-d4 hydrochloride	Inhibitor	99.16%	Unkown
HY-118046	GSK2163632A	Inhibitor	/	Unkown
HY-119232	GSK466317A	Inhibitor	/	Unkown
HY-123254	CCG-224406	Inhibitor	/	Unkown
HY-120718	CCG 224061	Inhibitor	/	Unkown
HY-168971	Paeoniflorin-6′-O-benzene sulfonate	Inhibitor	/	Unkown
HY-RS16845	Grk2 Mouse Pre-designed siRNA Set A	Inhibitor	/	Unkown
HY-RS23286	Grk2 Rat Pre-designed siRNA Set A	Inhibitor	/	Unkown
HY-180583	GRK5-IN-5	Inhibitor	/	Unkown

Orthologs Information

Species	Symbol	Source	ID
Homo sapiens	Grk2	NCBI	NCBI:156