GRK2 - G protein-coupled receptor kinase 2 Gene

Homo sapiens

Also known as BARK1; ADRBK1; BETA-ARK1

Gene ID: 156 | Gene type: protein coding

About GRK2

Cytogenetic location: 11q13.2 Genomic coordinates (GRCh38): 11:67,266,473-67,286,556 (from NCBI)

This gene has 14 transcripts (splice variants), 128 orthologues and 7 paralogues. Broad expression in bone marrow (RPKM 91.8), spleen (RPKM 61.9) and 24 other tissues.

Summary

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. Elevated expression of this gene has been observed in human patients with heart failure and Alzheimer's disease. [provided by RefSeq, Sep 2017]

GRK2 Products(1)

mRNA	Protein	Name
NM_001619.5	NP_001610.2	beta-adrenergic receptor kinase 1

Gene Ontology

Molecular Function
Biological Process
Cellular Component

Molecular Function GO Annotation	Evidence	Reference	Source
enables Edg-2 lysophosphatidic acid receptor binding	IDA IDA: Inferred from direct assay	19306925	GOA
enables G protein-coupled receptor kinase activity	IMP IMP: Inferred from mutant phenotype	15102938	GOA
enables protein binding	IPI IPI: Inferred from physical interaction	17006543	GOA
enables protein kinase activity	IMP IMP: Inferred from mutant phenotype	21983013	GOA

Biological Process GO Annotation	Evidence	Reference	Source
involved in cardiac muscle contraction	IMP IMP: Inferred from mutant phenotype	15051637	GOA
involved in desensitization of G protein-coupled receptor signaling pathway	IMP IMP: Inferred from mutant phenotype	15102938	GOA
involved in negative regulation of relaxation of smooth muscle	IMP IMP: Inferred from mutant phenotype	30284927	GOA
involved in negative regulation of striated muscle contraction	IMP IMP: Inferred from mutant phenotype	15051637	GOA
involved in negative regulation of the force of heart contraction by chemical signal	IMP IMP: Inferred from mutant phenotype	15051637	GOA
involved in receptor internalization	IDA IDA: Inferred from direct assay	20074556	GOA
involved in symbiont entry into host cell	IMP IMP: Inferred from mutant phenotype	23029581	GOA
involved in tachykinin receptor signaling pathway	IDA IDA: Inferred from direct assay	17986524	GOA
involved in viral genome replication	IMP IMP: Inferred from mutant phenotype	23029581	GOA

Cellular Component GO Annotation	Evidence	Reference	Source
located in cytoplasm	IDA IDA: Inferred from direct assay	17986524	GOA
located in cytoplasmic side of mitochondrial outer membrane	IDA IDA: Inferred from direct assay	21983013	GOA
located in cytosol	IDA IDA: Inferred from direct assay	21983013	GOA

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

GRK2 Protein Structure

RGS

Pkinase

0
200
400
600
689 a.a.

Protein Preferred Names

Protein Names

beta-adrenergic receptor kinase 1

adrenergic beta receptor kinase 1

GRK2 Protein-protein interaction Information

Type Cross Intra	Protein Name	Protein ID	Interactor	Interactor Species	Interactor ID	Detection Method	Reference
Intra	GRK2	P25098	NCAM1	Homo sapiens	P13591	Validated Y2H	32814053
Intra	GRK2	P25098	NCAM1	Homo sapiens	P13591	Y2H Array	32814053
Intra	GRK2	P25098	NCAM1	Homo sapiens	P13591	Y2H Pooling	32814053
Intra	GRK2	P25098	FPR1	Homo sapiens	P21462	Anti Bait CoIP	22447027
Intra	GRK2	P25098	GRK3	Homo sapiens	P35626	Anti Tag CoIP	28514442
Intra	GRK2	P25098	GRK3	Homo sapiens	P35626	Anti Tag CoIP	33961781
Intra	GRK2	P25098	GRK3	Homo sapiens	P35626	TAP	23455922
Intra	GRK2	P25098	UBC	Homo sapiens	P0CG48	Anti Bait CoIP	17006543
Intra	GRK2	P25098	UBC	Homo sapiens	P0CG48	Anti Tag CoIP	17006543
Intra	GRK2	P25098	MDM2	Homo sapiens	Q00987	Anti Bait CoIP	17006543
Intra	GRK2	P25098	ERBB3	Homo sapiens	P21860	Validated Y2H	32814053
Intra	GRK2	P25098	ERBB3	Homo sapiens	P21860	Y2H Array	32814053
Intra	GRK2	P25098	ERBB3	Homo sapiens	P21860	Y2H Pooling	32814053
Intra	GRK2	P25098	CSNK1D	Homo sapiens	P48730-2	Y2H Pooling	32814053
Intra	GRK2	P25098	CSNK1D	Homo sapiens	P48730-2	Validated Y2H	32814053
Intra	GRK2	P25098	CSNK1D	Homo sapiens	P48730-2	Y2H Array	32814053

Cross: Cross-species interaction Intra: Intraspecies interaction

Related Diseases

Diseases

Alias

Asphyxiating Thoracic Dystrophy

Jeune Thoracic Dystrophy	Jeune Syndrome
Asphyxiating Thoracic Dysplasia	Short-Rib Thoracic Dysplasia With Or Without Polydactyly
Thoracic Pelvic Phalangeal Dystrophy	Asphyxiating Thoracic Chondrodystrophy
Atd	Chondroectodermal Dysplasia-Like Syndrome
Infantile Thoracic Dystrophy	Jeune Thoracic Dysplasia
Thoracic Asphyxiant Dystrophy	Thoracic-Pelvic-Phalangeal Dystrophy
Short-Rib Thoracic Dysplasia Without Polydactyly	Asphyxiating Thoracic Dystrophy Of The Newborn
Asphyxiating Thorax Dystrophy

Short-Rib Thoracic Dysplasia 1 With Or Without Polydactyly

Asphyxiating Thoracic Dystrophy 1	Jeune Syndrome
SRTD1	Atd1
Asphyxiating Thoracic Dystrophy Of The Newborn	Jatd
Jeune Asphyxiating Thoracic Dystrophy	Thoracic-Pelvic-Phalangeal Dystrophy
Atd	Asphyxiating Thoracic Dystrophy
Chondroectodermal Dysplasia-Like Syndrome	Infantile Thoracic Dystrophy
Jeune'S Syndrome	Thoracic Pelvic Phalangeal Dystrophy
Jeune Thoracic Dystrophy

Heart Disease

Heart Failure	Congenital Heart Disease
Heart Diseases	Congenital Heart Defects
Congenital Heart Defect	Heart Malformation
Congenital Anomaly Of Heart	Heart Defect
Heart-Congenital Defect	Congenital Heart Disorder
Heart Defects Congenital	Heart Defects, Congenital
Heart Defects	Heart Disease, Congenital
Disease, Heart, Congenital	Congestive Heart Failure

Hypertension, Essential

Essential Hypertension	Hypertension
High Blood Pressure	Hypertension, Essential, Susceptibility To
Hypertensive Disease	Primary Hypertension
EHT	Hypertension, Salt-Sensitive Essential, Susceptibility To
Hyperpiesia	Idiopathic Hypertension
Hypertensive Disorder	Hypertension, Essential, Susceptibility To, 3
Hypertension, Essential 3	Hypertension, Essential, Salt-Sensitive
Hypertension, Essential, Susceptibility To, 6	Hypertension, Essential 6
Hypertension, Salt-Sensitive Essential	Hypertension, Susceptibility To
Hypertension, Essential, Susceptibility To, 4	Hypertension, Essential 4
Hypertension, Essential, Susceptibility To, 2	Hypertension, Essential 2
Hypertension, Essential, Susceptibility To, 1	Hypertension, Essential 1
Hypertension, Essential, Susceptibility To, 5	Hypertension, Essential 5
Htn	Vascular Hypertensive Disorder
Systemic Primary Arterial Hypertension	Hbp - [High Blood Pressure]
Systemic Arterial Hypertensive Disorder	Elevated Blood Pressure
Arterial Hypertension Nos	Hypertension Nos
Benign Hypertension	Systemic Arterial Hypertension
Systemic Hypertension	Artery Htn
Benign Htn	Vascular Htn
Vascular Hypertension	Cholesterol Hypertension
Cholesterol Htn	Idiopathic Htn
Malignant Hypertension	Malignant Htn
Raised Blood Pressure	Cardiovascular Hypertension
Primary Htn - [Hypertension]	High Arterial Tension
High Blood Pressure Disorder	Ht - [Hypertension]
Htn - [Hypertension]	Hypertensive Vascular Disease
Hypertensive Vascular Degeneration

Myocardial Infarction

Heart Attack	Myocardial Infarction, Susceptibility To
Myocardial Infarction 1	Myocardial Infarction, Protection Against
Myocardial Infarction, Decreased Susceptibility To	Myocardial Infarction, Decreased
Myocardial Infarct	MCI1
Premature Myocardial Infarction	Myocardial Infarction, Susceptibility To, Type 1

Colorectal Cancer

Colon Cancer	Colorectal Carcinoma
Colon Carcinoma	Colorectal Cancer, Susceptibility To
Carcinoma Of Colon	CRC
Colorectal Cancer With Chromosomal Instability, Somatic	Colon Cancer, Somatic
Colon Cancer, Susceptibility To	Colonic Neoplasms
Colorectal Neoplasms	Colorectal Cancer, Somatic
Colon Cancer, Advanced, Somatic	Colonic Carcinoma
Colorectal Carcinomas	Colon Cancers
Colorectal Cancers	Cancer, Colorectal, Somatic
Cancer, Colon	Cancer, Colorectal, Susceptibility To
Colorectal Neoplasm	Colonic Neoplasm
Malignant Tumor Of Colon

Dilated Cardiomyopathy

Familial Dilated Cardiomyopathy	Primary Dilated Cardiomyopathy
Idiopathic Dilated Cardiomyopathy	Congestive Cardiomyopathy
Idiopathic Dilation Cardiomyopathy	Primary Familial Dilated Cardiomyopathy
Cardiomyopathy, Dilated	DCM
Cardiomyopathy, Familial Dilated	Dilated Cardiomyopathy, Familial
Hypokinetic Dilated Cardiomyopathy, Familial	Familial Idiopathic Cardiomyopathy
Fdc	Cardiomyopathy, Familial Idiopathic
Idiopathic Cardiomegaly	Dilated Congestive Cardiomyopathy
Chronic Dilated Cardiomyopathy	Ccm - [Congestive Cardiomyopathy]
Cocm - [Congestive Cardiomyopathy]	Dcm - [Dilated Cardiomyopathy]
Dilated-Hypokinetic Cardiomyopathy	Congestive Idiopathic Cardiomyopathy
Primary Idiopathic Dilated Cardiomyopathy

Diseases	Alias
Waldenstroem'S Macroglobulinemia	Waldenstroem'S Macroglobulinemia Waldenstroem'S Macroglobulinemia Macroglobulinemia Of Waldenstrom Lymphoplasmacytic Lymphoma With Igm Gammopathy Lymphoplasmacytic Lymphoma Waldenstroem'S Macroglobulinemia Waldenstroem'S Macroglobulinemia Macroglobulinemia Of Waldenstrom Lymphoplasmacytic Lymphoma With Igm Gammopathy Lymphoplasmacytic Lymphoma

Related Agents

Approval

Bioactive Molecules (2)

Cat. No.	Product Name	Effect	Purity	Rare Diseases
HY-B0492	Paroxetine hydrochloride		99.96%	Unkown
HY-B0492A	Paroxetine hydrochloride hemihydrate		99.96%	Unkown

Pre-clinical Phase

Bioactive Molecules (24)

Cat. No.	Product Name	Effect	Purity	Rare Diseases
HY-112779	Pertussis Toxin		≥99.0%	Unkown
HY-103045	CMPD101	Inhibitor	98.95%	Unkown
HY-W013411A	Locostatin	Inhibitor	99.82%	Unkown
HY-109562A	CCG258208 hydrochloride		98.05%	Unkown
HY-18991	CCG215022	Inhibitor	98.69%	Unkown
HY-18990	GSK180736A	Inhibitor	98.01%	Unkown
HY-47573	CCG273441	Inhibitor	98.67%	Unkown
HY-156863	GRK2 Inhibitor 2	Inhibitor	98.88%	Unkown
HY-139690	CCG258747	Inhibitor	99.17%	Unkown
HY-123538	GRK2 Inhibitor 1	Inhibitor	98.03%	Unkown
HY-P1396A	GRK2i TFA	Inhibitor	98.41%	Unkown
HY-129118	Takeda103A		98.69%	Unkown
HY-109562	CCG258208		/	Unkown
HY-118046	GSK2163632A	Inhibitor	/	Unkown
HY-119232	GSK466317A	Inhibitor	/	Unkown
HY-150022	GRK5-IN-4	Inhibitor	/	Unkown
HY-150039	CCG-271423	Inhibitor	/	Unkown
HY-151216S	rel-Paroxetine-d4 hydrochloride		/	Unkown
HY-155099	FGH31	Agonist	/	Unkown
HY-B0492S1	Paroxetine-d4 hydrochloride		99.16%	Unkown
HY-P1396	GRK2i	Inhibitor	/	Unkown
HY-RS05813	GRK2 Human Pre-designed siRNA Set A	Pre-designed Sets	/	Unkown
HY-103045A	CMPD101 hydrochloride	Inhibitor	/	Unkown
HY-123254	CCG-224406	Inhibitor	/	Unkown

Orthologs Information

Species	Symbol	Source	ID
Macaca mulatta	GRK2	VGNC	VGNC:73253
Rattus norvegicus	GRK2	RGD	RGD:2062
Mus musculus	GRK2	MGD	MGI:87940
Canis familiaris	GRK2	VGNC	VGNC:41502
Bos taurus	GRK2	VGNC	VGNC:56266
Felis catus	GRK2	VGNC	VGNC:62718

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