Tchem APLNR Apelin receptor

Protein Summary

Description

Receptor for apelin receptor early endogenous ligand (APELA) and apelin (APLN) hormones coupled to G proteins that inhibit adenylate cyclase activity (PubMed:11090199, PubMed:25639753, PubMed:28137936). Plays a key role in early development such as gastrulation, blood vessels formation and heart morphogenesis by acting as a receptor for APELA hormone (By similarity). May promote angioblast migration toward the embryonic midline, i.e. the position of the future vessel formation, during vasculogenesis (By similarity). Promotes sinus venosus (SV)-derived endothelial cells migration into the developing heart to promote coronary blood vessel development (By similarity). Plays also a role in various processes in adults such as regulation of blood vessel formation, blood pressure, heart contractility and heart failure (PubMed:25639753, PubMed:28137936). (Microbial infection) Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia (PubMed:11090199). This gene encodes a member of the G protein-coupled receptor gene family. The encoded protein is related to the angiotensin receptor, but is actually an apelin receptor that inhibits adenylate cyclase activity and plays a counter-regulatory role against the pressure action of angiotensin II by exerting hypertensive effect. It functions in the cardiovascular and central nervous systems, in glucose metabolism, in embryonic and tumor angiogenesis and as a human immunodeficiency virus (HIV-1) coreceptor. Two transcript variants resulting from alternative splicing have been identified. [provided by RefSeq, Jul 2009]

Uniprot Accession IDs

• P35414

Gene Name

• APLNR

Ensembl ID

• ENST00000257254
• ENSP00000257254
• ENSG00000134817
• ENST00000606794
• ENSP00000475344
• ENST00000611099
• ENSP00000477818

Symbol

• AGTRL1
• APJ
• APJ
• APJR
• HG11
• AGTRL1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
cell type or tissue	0.7
biological term	0.62
tissue sample	0.61
protein domain	0.58
ligand (chemical)	0.56

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class A Rhodopsin Like / Apelin Receptor / Apelin Receptor

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: 473.53   (req: < 5)

Gene RIFs: 72   (req: <= 3)

Antibodies: 517   (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: 473.53   (req: >= 5)

Gene RIFs: 72   (req: > 3)

Antibodies: 517   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 15

Tchem

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

Active Ligands: 102

Tclin

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

Active Drug: 0

Expression Data (0 Tissues)

tutorial

No expression data found

Protein Sequence and Structure

Residue Counts

Protein Sequence

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Related Tools (4)

Target Illumination GWAS Analytics (TIGA)

TIGA scores and ranks GWAS discovered associations according to the quantity and quality of the evidence supporting the association.

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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 (0)

No approved drugs found

Active Ligands (102)

Explore Active Ligands

1 – 10 of 102

AMG 986

APLNRTchem GPCR

pEC50 : 9.49

E339-3D6

APLNRTchem GPCR

-log(-) : 6.4

CMF-019

APLNRTchem GPCR

pEC50 : 10

CHEMBL4473347

APLNRTchem GPCR

pEC50 : 10.21

CHEMBL4639193

APLNRTchem GPCR

pEC50 : 10.15

CHEMBL4518406

APLNRTchem GPCR

pEC50 : 10.08

CHEMBL4435973

APLNRTchem GPCR

pEC50 : 10.03

CHEMBL4076049

APLNRTchem GPCR

pKi : 10

[Pyr1]apelin-13

APLNRTchem GPCR

pKi : 9.43

CHEMBL4299566

APLNRTchem GPCR

pKi : 9.85

Protein-Protein Interactions (362)

Explore Interacting Targets

1 – 10 of 362

• See Interactions on String-DB

AKR1D1

Tbio

Family:  Enzyme

Novelty:  0.01264297

p_int:  0.999984238

p_ni:  0.000015762

Data Source:  BioPlex

TTI2

Tdark

Novelty:  0.18394695

p_int:  0.999698678

p_ni:  0.000286428

p_wrong:  0.000014894

Data Source:  BioPlex

MCUB

Tbio

Novelty:  0.0486243

p_int:  0.999471081

p_ni:  0.000528919

Data Source:  BioPlex

SLC25A24

Tbio

Family:  Transporter

Novelty:  0.06151955

p_int:  0.999409021

p_ni:  0.000590972

p_wrong:  6e-9

Data Source:  BioPlex

ORC5

Tbio

Novelty:  0.02264865

p_int:  0.998716289

p_ni:  0.001283698

p_wrong:  1.3e-8

Data Source:  BioPlex

TMEM161B

Tbio

Novelty:  0.27823549

p_int:  0.998468655

p_ni:  0.001531338

p_wrong:  8e-9

Data Source:  BioPlex

PDS5B

Tbio

Novelty:  0.00295057

p_int:  0.996954768

p_ni:  0.003045232

Data Source:  BioPlex

ABCD1

Tbio

Family:  Transporter

Novelty:  0.0067013

p_int:  0.996502309

p_ni:  0.003412851

p_wrong:  0.00008484

Data Source:  BioPlex

ADCK1

Tchem

Family:  Kinase

Novelty:  0.31158074

p_int:  0.996376839

p_ni:  0.003622713

p_wrong:  4.47e-7

Data Source:  BioPlex

HIP1R

Tbio

Novelty:  0.02502713

p_int:  0.995500592

p_ni:  0.004499408

Data Source:  BioPlex

Nearest Tclin Targets

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

Pathways (10)

Reactome (7)

KEGG (2)

WikiPathways (1)

Class A/1 (Rhodopsin-like receptors) (R-HSA-373076)

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Data Source	Name	Explore in Pharos	Explore in Source
Reactome	Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
Reactome	G alpha (i) signalling events	408 targets	R-HSA-418594
Reactome	GPCR downstream signalling	1152 targets	R-HSA-388396
Reactome	GPCR ligand binding	460 targets	R-HSA-500792
Reactome	Peptide ligand-binding receptors	189 targets	R-HSA-375276

Name	Explore in Pharos	Explore in Source
Class A/1 (Rhodopsin-like receptors)	323 targets	R-HSA-373076
G alpha (i) signalling events	408 targets	R-HSA-418594
GPCR downstream signalling	1152 targets	R-HSA-388396
GPCR ligand binding	460 targets	R-HSA-500792
Peptide ligand-binding receptors	189 targets	R-HSA-375276

Viral Interactions (0)

No viral interactions found

Gene Ontology Terms (17)

Functions (2)

Components (2)

Processes (13)

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GO Term	Evidence	Assigned by
G protein-coupled receptor activity	Traceable Author Statement (TAS)	ProtInc
signaling receptor activity	Traceable Author Statement (TAS)	ProtInc

Disease Associations (null)

No disease associations found

GWAS Traits (6)

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GWAS Trait	EFO ID	Study Count	SNP Count	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
mean corpuscular volume	EFO_0004526	1	1	1		53.3
apolipoprotein A 1 measurement	EFO_0004614	1	1	1		11.6
high density lipoprotein cholesterol measurement	EFO_0004612	1	1	1		7.8
heel bone mineral density	EFO_0009270	1	1	1		6.7
body mass index	EFO_0004340	1	1	1		2.6

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GWAS Trait	EFO ID	Beta Count	Odds Ratio	Evidence (Mean Rank Score)	Provenance
mean corpuscular volume	EFO_0004526	1		53.3
apolipoprotein A 1 measurement	EFO_0004614	1		11.6
high density lipoprotein cholesterol measurement	EFO_0004612	1		7.8
heel bone mineral density	EFO_0009270	1		6.7
body mass index	EFO_0004340	1		2.6

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Find similar targets by:

UniProt Keyword Find Similar Targets

No Header	No Header
3D-structure
Angiogenesis
Cell membrane
Complete proteome
Developmental protein
G-protein coupled receptor
Gastrulation
Glycoprotein
Membrane
Polymorphism

GWAS Trait Find Similar Targets

No Header	No Header
apolipoprotein A 1 measurement
body mass index
heel bone mineral density
high density lipoprotein cholesterol measurement
mathematical ability
mean corpuscular volume

MGI Phenotype Find Similar Targets

No Header	No Header
behavior/neurological phenotype
cardiovascular system phenotype
embryo phenotype
endocrine/exocrine gland phenotype
growth/size/body region phenotype
homeostasis/metabolism phenotype
mortality/aging
muscle phenotype
renal/urinary system phenotype
reproductive system phenotype

IDG Resources

No IDG generated resources found

Orthologs (12)

1 – 5 of 12

Species	Name	Source ID	Gene ID	OMA	EggNOG	Inparanoid
Chimp	apelin receptor	VGNC:53053	466585
Macaque	apelin receptor		706823
Mouse	apelin receptor	MGI:1346086	23796
Rat	apelin receptor	RGD:621645	83518
Dog	apelin receptor	VGNC:37987	483497

Species	Name	OMA	EggNOG	Inparanoid
Chimp	apelin receptor
Macaque	apelin receptor
Mouse	apelin receptor
Rat	apelin receptor
Dog	apelin receptor

Publication Statistics

PubMed Score 473.53

PubMed score by year

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PubTator Score 199.84

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Patents

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Related Publications

Text Mined References (88)

GeneRif Annotations (72)

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PMID	Year	Title