Tchem ABCG2 ATP-binding cassette sub-family G member 2

Protein Summary

Description

High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. Implicated in the efflux of numerous drugs and xenobiotics: mitoxantrone, the photosensitizer pheophorbide, camptothecin, methotrexate, azidothymidine (AZT), and the anthracyclines daunorubicin and doxorubicin. The membrane-associated protein encoded by this gene is included in the superfamily of ATP-binding cassette (ABC) transporters. ABC proteins transport various molecules across extra- and intra-cellular membranes. ABC genes are divided into seven distinct subfamilies (ABC1, MDR/TAP, MRP, ALD, OABP, GCN20, White). This protein is a member of the White subfamily. Alternatively referred to as a breast cancer resistance protein, this protein functions as a xenobiotic transporter which may play a major role in multi-drug resistance. It likely serves as a cellular defense mechanism in response to mitoxantrone and anthracycline exposure. Significant expression of this protein has been observed in the placenta, which may suggest a potential role for this molecule in placenta tissue. Multiple transcript variants encoding different isoforms have been found for this gene. [provided by RefSeq, Apr 2012]

Uniprot Accession IDs

• Q9UNQ0
• A0A1W3
• A8K1T5
• O95374
• Q4W5I3
• Q53ZQ1
• Q569L4
• Q5YLG4
• Q86V64
• Q8IX16
• Q96LD6
• Q96TA8
• Q9BY73
• Q9NUS0

Gene Name

• ABCG2

Ensembl ID

• ENST00000237612
• ENSP00000237612
• ENSG00000118777
• ENST00000515655
• ENSP00000426917

Symbol

• ABCP
• BCRP
• BCRP1
• MXR
• MRX
• MXR
• ABCP
• BCRP
• BMDP
• MXR1
• ABC15
• BCRP1
• CD338
• GOUT1
• MXR-1
• CDw338
• UAQTL1
• EST157481

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
chemical	1
drug	1
molecular function	1
disease	0.9
histone modification site profile	0.86

Protein Classes

PANTHER Classes

Protein / Transporter / Atp-binding Cassette (Abc) Transporter / Atp-binding Cassette Sub-family G Member 2

DTO Classes

Protein / Transporter / Atp-binding Cassette Transporter Family / Abcg Subfamily / Atp-binding Cassette Sub-family G Member 2

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 3883.46   (req: < 5)

Gene RIFs: 677   (req: <= 3)

Antibodies: 322   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 3883.46   (req: >= 5)

Gene RIFs: 677   (req: > 3)

Antibodies: 322   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 13

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 537

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 6

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Expression Data (0 Tissues)

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No expression data found

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Target Illumination GWAS Analytics (TIGA)

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GENEVA

GENEVA (GENe Expression Variance Analysis) allows you to identify RNA-sequencing datasets from the Gene Expression Omnibus (GEO) that contain conditions modulating a gene or a gene signature.

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GlyGen

GlyGen is a data integration and dissemination project for carbohydrate and glycoconjugate related data.

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ARCHS4

ARCHS4 provides access to gene-function predictions based on RNA-seq co-expression, and gene expression levels across cell and tissues.

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Approved Drugs (6)

Explore Approved Drugs

1 – 6 of 6

imatinib

ABCG2Tchem Transporter

INHIBITOR pKd : 7.89

verapamil

ABCG2Tchem Transporter

BLOCKER pIC50 : 5

quercetin

ABCG2Tchem Transporter

pKd : 7.6

mitoxantrone

ABCG2Tchem Transporter

INHIBITOR pIC90 : 5.96

diethylstilbestrol

ABCG2Tchem Transporter

AGONIST pKi : 9.66

gefitinib

ABCG2Tchem Transporter

INHIBITOR pKi : 9.4

Active Ligands (537)

Explore Active Ligands

1 – 10 of 537

JAK3 inhibitor II

ABCG2Tchem Transporter

pIC50 : 8.4

EKI-785

ABCG2Tchem Transporter

pIC50 : 9.7

Linsitinib

ABCG2Tchem Transporter

pKd : 8

CHEMBL4286793

ABCG2Tchem Transporter

pEC50 : 8.19

CHEMBL539987

ABCG2Tchem Transporter

pKi : 6.7

CHEMBL4282529

ABCG2Tchem Transporter

pEC50 : 7.11

CHEMBL4280256

ABCG2Tchem Transporter

pEC50 : 7.61

CHEMBL4278382

ABCG2Tchem Transporter

pEC50 : 7.42

CHEMBL4286968

ABCG2Tchem Transporter

pEC50 : 7.77

CHEMBL4291291

ABCG2Tchem Transporter

pEC50 : 8.51

Protein-Protein Interactions (224)

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1 – 10 of 224

• See Interactions on String-DB

TRIM13

Tbio

Family:  Enzyme

Novelty:  0.00085649

p_int:  0.999953152

p_ni:  0.000046638

p_wrong:  2.1e-7

Data Source:  BioPlex

SCAMP1

Tbio

Novelty:  0.03293648

p_int:  0.969154338

p_ni:  0.030443828

p_wrong:  0.000401835

Data Source:  BioPlex

CLPP

Tchem

Family:  Enzyme

Novelty:  0.00105289

p_int:  0.959667742

p_ni:  0.040332258

Data Source:  BioPlex

CD55

Tbio

Novelty:  0.0005689

p_int:  0.948557248

p_ni:  0.050592219

p_wrong:  0.000850534

Data Source:  BioPlex

SLC19A2

Tbio

Family:  Transporter

Novelty:  0.00761796

p_int:  0.894884576

p_ni:  0.093234179

p_wrong:  0.011881244

Score:  0.177

Data Source:  BioPlex,STRINGDB

LGALS3

Tchem

Novelty:  0.00032754

p_int:  0.89372036

p_ni:  0.10627964

Score:  0.199

Data Source:  BioPlex,STRINGDB

SRC

Tclin

Family:  Kinase

Novelty:  0.00008479

p_int:  0.879097668

p_ni:  0.12090113

p_wrong:  0.000001202

Score:  0.403

Data Source:  BioPlex,STRINGDB

ATP5F1B

Tbio

Family:  Enzyme

Novelty:  0.01053177

p_int:  0.813079889

p_ni:  0.186920111

Data Source:  BioPlex

VTA1

Tbio

Novelty:  0.01697854

p_int:  0.766115775

p_ni:  0.23384155

p_wrong:  0.000042675

Data Source:  BioPlex

ABCC1

Tchem

Family:  Transporter

Novelty:  0.00119837

Score:  0.943

Data Source:  STRINGDB

Nearest Tclin Targets

Nearest Tclin calculations are only available for targets with KEGG Pathway annotations.

Pathways (30)

Reactome (5)

KEGG (3)

PathwayCommons (2)

WikiPathways (20)

Abacavir transmembrane transport (R-HSA-2161517)

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Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Abacavir transmembrane transport	5 targets	R-HSA-2161517
Reactome	Abacavir transport and metabolism	10 targets	R-HSA-2161522
Reactome	Iron uptake and transport	59 targets	R-HSA-917937
Reactome	Metabolism	2112 targets	R-HSA-1430728
Reactome	Transport of small molecules	725 targets	R-HSA-382551

Name	Explore in Pharos	Explore in Source
Abacavir transmembrane transport	5 targets	R-HSA-2161517
Abacavir transport and metabolism	10 targets	R-HSA-2161522
Iron uptake and transport	59 targets	R-HSA-917937
Metabolism	2112 targets	R-HSA-1430728
Transport of small molecules	725 targets	R-HSA-382551

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (19)

Functions (8)

Components (6)

Processes (5)

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1 – 8 of 8

GO Term	Evidence	Assigned by
protein homodimerization activity	Inferred from Direct Assay (IDA)	BHF-UCL
identical protein binding	Inferred from Physical Interaction (IPI)	IntAct
ATPase activity, coupled to transmembrane movement of substances	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
drug transmembrane transporter activity	Inferred from Biological aspect of Ancestor (IBA)	GO_Central
ATP binding	Traceable Author Statement (TAS)	ProtInc
heme transporter activity	Traceable Author Statement (TAS)	Reactome
transporter activity	Traceable Author Statement (TAS)	ProtInc
xenobiotic transmembrane transporting ATPase activity	Traceable Author Statement (TAS)	ProtInc

Disease Associations ()

No disease associations found

GWAS Traits (33)

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1 – 5 of 33

GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
urate measurement	EFO_0004531	13	19	29	6	99.9
uric acid measurement	EFO_0004761	13	8	18	1.9	99.4
gout	EFO_0004274	15	8	0	1.9	99.2
amino acid measurement	EFO_0005134	4	4	5		94.1
blood metabolite measurement	EFO_0005664	2	4	6		94.1

• Explore on Target Illumination GWAS Analytics (TIGA)

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1 – 5 of 33

GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
urate measurement	EFO_0004531	29	6	99.9
uric acid measurement	EFO_0004761	18	1.9	99.4
gout	EFO_0004274	0	1.9	99.2
amino acid measurement	EFO_0005134	5		94.1
blood metabolite measurement	EFO_0005664	6		94.1

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UniProt Keyword Find Similar Targets

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3D-structure
Alternative splicing
ATP-binding
Cell membrane
Complete proteome
Disulfide bond
Glycoprotein
Membrane
Mitochondrion
Nucleotide-binding

GWAS Trait Find Similar Targets

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alkaline phosphatase measurement
amino acid measurement
aspartate aminotransferase measurement
bitter beverage consumption measurement
blood metabolite measurement
body height
body mass index
butyrylcholinesterase measurement
C-reactive protein measurement
coffee consumption measurement

MGI Phenotype Find Similar Targets

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adipose tissue phenotype
behavior/neurological phenotype
cellular phenotype
hematopoietic system phenotype
homeostasis/metabolism phenotype
immune system phenotype
integument phenotype
liver/biliary system phenotype
renal/urinary system phenotype

IDG Resources

No IDG generated resources found

Orthologs (11)

1 – 5 of 11

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	ATP binding cassette subfamily G member 2	VGNC:2951	471251
Macaque	ATP binding cassette subfamily G member 2 (Junior blood group)		574307
Mouse	ATP binding cassette subfamily G member 2 (Junior blood group)	MGI:1347061	26357
Rat	ATP binding cassette subfamily G member 2	RGD:631345	312382
Dog	ATP binding cassette subfamily G member 2	VGNC:49113	478472

Species	Name	OMA	EggNOG	Inparanoid
Chimp	ATP binding cassette subfamily G member 2
Macaque	ATP binding cassette subfamily G member 2 (Junior blood group)
Mouse	ATP binding cassette subfamily G member 2 (Junior blood group)
Rat	ATP binding cassette subfamily G member 2
Dog	ATP binding cassette subfamily G member 2

Publication Statistics

PubMed Score 3883.46

PubMed score by year

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PubTator Score 2060.51

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Related Publications

Text Mined References (756)

GeneRif Annotations (677)

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PMID	Year	Title