GRK2 - G protein-coupled receptor kinase 2 Gene

Also Known as BARK1; ADRBK1; BETA-ARK1

Species: Homo sapiens

Gene Type: protein coding

Gene ID: 156

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	References	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	References	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	References	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	Protein Name	Protein ID	Interactor	Interactor Species	Interactor ID	Detection Method	References
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

GRK2 Antibodies

Cat. No.	Product Name	Application	Reactivity
HY-P83204	GRK2 Antibody (YA2949)	WB, IP	Human
HY-P83204A	GRK2 Antibody (YA2949)(PBS only)	WB, IP	Human
HY-P84209	GRK2 Antibody (YA3906)	WB, IHC-P, ICC/IF, ELISA	Human, Mouse, Rat, Monkey
HY-P84209A	GRK2 Antibody (YA3906)(PBS only)	WB, IHC-P, ICC/IF, ELISA	Human, Mouse, Rat, Monkey
HY-P85193	GRK2 Antibody (YA4885)	WB, IHC-P, FC	Human, Mouse, Rat
HY-P85534	GRK2 Antibody (YA5226)	WB	Human

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
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	98.96%	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
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
Others	GRK2	NCBI