| 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]
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
| NCBI Gene PubMed Count | 55 |
| Grant Count | 75 |
| R01 Count | 56 |
| Funding | $7,172,169.31 |
| PubMed Score | 237.02 |
| PubTator Score | 91.19 |
| Disease | log2 FC | p |
|---|---|---|
| interstitial lung disease | 1.200 | 0.048 |
| malignant mesothelioma | -2.000 | 0.000 |
| astrocytic glioma | -1.300 | 0.002 |
| osteosarcoma | 2.167 | 0.009 |
| medulloblastoma, large-cell | 2.400 | 0.002 |
| primary pancreatic ductal adenocarcinoma | 2.002 | 0.001 |
| intraductal papillary-mucinous adenoma (... | -2.300 | 0.007 |
| intraductal papillary-mucinous carcinoma... | -2.700 | 0.004 |
| intraductal papillary-mucinous neoplasm ... | -2.700 | 0.024 |
| Hydrolethalus syndrome | -2.566 | 0.036 |
| lung cancer | 4.000 | 0.000 |
| Breast cancer | 2.800 | 0.018 |
| ductal carcinoma in situ | -1.500 | 0.043 |
| pituitary cancer | 1.400 | 0.033 |
| pancreatic cancer | 1.800 | 0.001 |
CHEMBL388978
pKd 7.57
CHEMBL3321809
pKd 8.07
CHEMBL386051
pKd 8.12
CHEMBL2336005
pIC50 8.29
CHEMBL459850
pEC50 8.70
CHEMBL1784637
pIC50 8.92
CHEMBL1230609
pKd 9.00
CHEMBL249097
pKd 10.00
| PMID | Text |
|---|---|
| 26552734 | A novel association between the EPHA3 deletion and prostate cancer risk was observed in Finnish individuals. |
| 26381449 | This study showed that EPHA3 gene involved in neuronal growth and cerebellum development and associated with neurological and psychological disorders. |
| 26232493 | EphA3 forms dimers in the absence of ligand binding. |
| 25993310 | the structure of the ligand-binding domain of the EphA3 receptor in complex with its preferred ligand, ephrin-A5, is reported. |
| 25420155 | Data indicate that hypoxia increased EphA3 receptor (EphA3) mRNA expression in EphA3+ endometrial multipotent mesenchymal stromal cells (eMSCs). |
| 25231727 | EphA3 was induced by PC-1 and contributed to the malignant progression of prostate cancer |
| 23991104 | Based on the knowledge that EPHA4 has been previously shown to rescue SOD1 transgenic mice from ALS phenotype and prolongs survival, EPHA3 may be a promising candidate for therepuetic interventions |
| 23970317 | EphA3 may represent a novel candidate marker for patient prognosis as well a molecular target for HCC therapy. |
| 23410976 | High EphA3 expression is associated with glioblastoma multiforme. |
| 23324396 | EPHA3 mutations may promote tumorigenesis only when key senescence-inducing pathways have been inactivated. |
| More... |
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 //
| PMID | Year | Title |
|---|---|---|
| 26552734 | 2016 | Germline copy number variation analysis in Finnish families with hereditary prostate cancer. |
| 26381449 | 2015 | The association of DNA methylation and brain volume in healthy individuals and schizophrenia patients. |
| 26232493 | 2015 | Unliganded EphA3 dimerization promoted by the SAM domain. |
| 25993310 | 2015 | Distinctive Structure of the EphA3/Ephrin-A5 Complex Reveals a Dual Mode of Eph Receptor Interaction for Ephrin-A5. |
| 25420155 | 2014 | Hypoxia-controlled EphA3 marks a human endometrium-derived multipotent mesenchymal stromal cell that supports vascular growth. |
| 25231727 | 2014 | EphA3, induced by PC-1/PrLZ, contributes to the malignant progression of prostate cancer. |
| 24024966 | 2013 | Genome-wide association study of chronic periodontitis in a general German population. |
| 23991104 | 2013 | Genome-wide copy number variation in sporadic amyotrophic lateral sclerosis in the Turkish population: deletion of EPHA3 is a possible protective factor. |
| 23970317 | 2013 | High levels of EphA3 expression are associated with high invasive capacity and poor overall survival in hepatocellular carcinoma. |
| 23410976 | 2013 | EphA3 maintains tumorigenicity and is a therapeutic target in glioblastoma multiforme. |
| More... |
