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  7. Ephrin type-A receptor 3

Tchem Ephrin type-A receptor 3

Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin family ligands residing on adjacent cells, leading to contact-dependent bidirectional signaling into neighboring cells. The signaling pathway downstream of the receptor is referred to as forward signaling while the signaling pathway downstream of the ephrin ligand is referred to as reverse signaling. Highly promiscuous for ephrin-A ligands it binds preferentially EFNA5. Upon activation by EFNA5 regulates cell-cell adhesion, cytoskeletal organization and cell migration. Plays a role in cardiac cells migration and differentiation and regulates the formation of the atrioventricular canal and septum during development probably through activation by EFNA1. Involved in the retinotectal mapping of neurons. May also control the segregation but not the guidance of motor and sensory axons during neuromuscular circuit development.

This gene belongs to the ephrin receptor subfamily of the protein-tyrosine kinase family. EPH and EPH-related receptors have been implicated in mediating developmental events, particularly in the nervous system. Receptors in the EPH subfamily typically have a single kinase domain and an extracellular region containing a Cys-rich domain and 2 fibronectin type III repeats. The ephrin receptors are divided into 2 groups based on the similarity of their extracellular domain sequences and their affinities for binding ephrin-A and ephrin-B ligands. This gene encodes a protein that binds ephrin-A ligands. Two alternatively spliced transcript variants have been described for this gene. [provided by RefSeq, Jul 2008]

 Comments

Property Summary

Ligand Count 16
NCBI Gene PubMed Count 59
PubMed Score 248.54
PubTator Score 91.19

Knowledge Summary

Patent (35,988)

TINX Plot

  Disease (5)

Disease Target Count Z-score Confidence
Carcinoma 11493 0.0 1.4
Kidney cancer 2613 0.0 1.1
Skin cancer 469 0.0 0.5
Disease Target Count Z-score Confidence
Orofacial cleft 54 0.0 3.0

Expression

  Differential Expression (15)

Disease log2 FC p
lung cancer 4.000 7.4e-06
Breast cancer 2.300 2.7e-02
astrocytic glioma -1.300 2.4e-03
ductal carcinoma in situ -1.500 4.3e-02
Hydrolethalus syndrome -2.566 3.6e-02
interstitial lung disease 1.200 4.8e-02
intraductal papillary-mucinous adenoma (... -2.300 6.7e-03
intraductal papillary-mucinous carcinoma... -2.700 3.8e-03
intraductal papillary-mucinous neoplasm ... -2.700 2.4e-02
malignant mesothelioma -2.000 3.9e-05
medulloblastoma, large-cell 2.000 2.0e-02
osteosarcoma 2.167 9.2e-03
pancreatic cancer 1.800 8.9e-04
pituitary cancer 1.400 3.3e-02
primary pancreatic ductal adenocarcinoma 2.002 1.4e-03

Synonym

Accession P29320 Q9H2V3 Q9H2V4
Symbols EK4
ETK
HEK
ETK1
HEK4
TYRO4

Gene

EPHA3

  Ortholog (12)

Species Source Disease
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
Inparanoid OMA EggNOG
OMA EggNOG
Inparanoid OMA
Inparanoid OMA
OMA EggNOG
Inparanoid OMA EggNOG

 UniProt Keyword (22)

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 GO Function (2)

 GO Component (4)

 GO Process (15)

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 Compartment GO Term (27)

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 MGI Phenotype (6)

 GWAS Trait (5)

 HCA RNA Cell Line (51)

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 CSPA Cell Line (6)

Pathway (10)

PDB (27)

Drug (1)

Structure of dasatinib

dasatinib
pKd 10.03

Ligand (15)

Structure of dasatinib

dasatinib
pKd 10.03

Structure of bosutinib

bosutinib
pKd 8.24

Structure of CHEMBL388978

CHEMBL388978
pKd 7.57

Structure of CHEMBL3321809

CHEMBL3321809
pKd 8.07

Structure of CHEMBL386051

CHEMBL386051
pKd 8.12

Structure of CHEMBL288441

CHEMBL288441
pKd 8.24

Structure of CHEMBL2336005

CHEMBL2336005
pIC50 8.29

Structure of CHEMBL459850

CHEMBL459850
pEC50 8.70

Structure of CHEMBL1784637

CHEMBL1784637
pIC50 8.92

Structure of CHEMBL1230609

CHEMBL1230609
pKd 9.00

Structure of CHEMBL249097

CHEMBL249097
pKd 10.00

Structure of compound 20 [PMID: 23489211]

compound 20 [PMID: 23489211]
pIC50 5.60

Structure of compound 66 [PMID: 19788238]

compound 66 [PMID: 19788238]
pIC50 7.40

Structure of compound 8h [PMID: 21561767]

compound 8h [PMID: 21561767]
pIC50 8.92

Structure of sitravatinib

sitravatinib
pIC50 9.00

Gene RIF (30)

AA Sequence 

MDCQLSILLLLSCSVLDSFGELIPQPSNEVNLLDSKTIQGELGWISYPSHGWEEISGVDEHYTPIRTYQV      1 - 70
CNVMDHSQNNWLRTNWVPRNSAQKIYVELKFTLRDCNSIPLVLGTCKETFNLYYMESDDDHGVKFREHQF     71 - 140
TKIDTIAADESFTQMDLGDRILKLNTEIREVGPVNKKGFYLAFQDVGACVALVSVRVYFKKCPFTVKNLA    141 - 210
MFPDTVPMDSQSLVEVRGSCVNNSKEEDPPRMYCSTEGEWLVPIGKCSCNAGYEERGFMCQACRPGFYKA    211 - 280
LDGNMKCAKCPPHSSTQEDGSMNCRCENNYFRADKDPPSMACTRPPSSPRNVISNINETSVILDWSWPLD    281 - 350
TGGRKDVTFNIICKKCGWNIKQCEPCSPNVRFLPRQFGLTNTTVTVTDLLAHTNYTFEIDAVNGVSELSS    351 - 420
PPRQFAAVSITTNQAAPSPVLTIKKDRTSRNSISLSWQEPEHPNGIILDYEVKYYEKQEQETSYTILRAR    421 - 490
GTNVTISSLKPDTIYVFQIRARTAAGYGTNSRKFEFETSPDSFSISGESSQVVMIAISAAVAIILLTVVI    491 - 560
YVLIGRFCGYKSKHGADEKRLHFGNGHLKLPGLRTYVDPHTYEDPTQAVHEFAKELDATNISIDKVVGAG    561 - 630
EFGEVCSGRLKLPSKKEISVAIKTLKVGYTEKQRRDFLGEASIMGQFDHPNIIRLEGVVTKSKPVMIVTE    631 - 700
YMENGSLDSFLRKHDAQFTVIQLVGMLRGIASGMKYLSDMGYVHRDLAARNILINSNLVCKVSDFGLSRV    701 - 770
LEDDPEAAYTTRGGKIPIRWTSPEAIAYRKFTSASDVWSYGIVLWEVMSYGERPYWEMSNQDVIKAVDEG    771 - 840
YRLPPPMDCPAALYQLMLDCWQKDRNNRPKFEQIVSILDKLIRNPGSLKIITSAAARPSNLLLDQSNVDI    841 - 910
TTFRTTGDWLNGVWTAHCKEIFTGVEYSSCDTIAKISTDDMKKVGVTVVGPQKKIISSIKALETQSKNGP    911 - 980
VPV                                                                       981 - 983
//

Text Mined References (64)

PMID Year Title