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Gene Review

EPHA3  -  EPH receptor A3

Homo sapiens

Synonyms: EK4, EPH-like kinase 4, ETK, ETK1, Eph-like tyrosine kinase 1, ...
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Disease relevance of EPHA3

  • We identified somatic mutations in GUCY2F, EPHA3, and NTRK3 in breast, lung, and pancreatic cancers [1].
  • We transfected a series of promoter deletion constructs into HepG2 (human hepatoma), H4 (rat hepatoma), and HEK (human embryonic kidney) cells and obtained maximal expression with 134 base pairs (bp) of 5'-flanking DNA [2].
  • This compound is able to raise O-GlcNAc levels in human HEK 293 and SH-SY5Y neuroblastoma cell lines and thus provides a novel, potent tool for the study of the role of O-GlcNAc in intracellular signal transduction pathways [3].
  • To facilitate reference, the gene was provisionally designated as 'RIK'. It was expressed in the HEK 293, one osteosarcoma (HOS), two carcinoma (COLO320 and QDMT), and three Burkitt lymphoma lines (BL2, BL29 and BL31) [4].
  • Virions released from infected NHP cells could productively infect naïve human cell lines, HEK 293 and HeLa, as shown by RT-PCR and RT assay [5].

High impact information on EPHA3

  • Also, blocking farnesylation of authentic progerin in transiently transfected HeLa, HEK 293, and NIH 3T3 cells with farnesyltransferase inhibitors (FTIs) restored normal nuclear architecture [6].
  • We identified substances present in HEK 293 and astrocyte cell extracts that strongly stimulate d-serine production by SR and elicit production of pyruvate [7].
  • The EPH-like receptor tyrosine kinase (RTK) HEK (human EPH-like kinase) was identified previously as a membrane antigen on the LK63 human pre-B-cell line and overexpression in leukemic specimens and cell lines suggested a role in oncogenesis [8].
  • We have previously shown that a monoclonal antibody (IIIA4) raised against LK63 recognized a glycosylated, cell-surface 135-kDa molecule (HEK), which displayed tyrosine kinase activity in vitro [9].
  • COS cells transfected with the sense HEK/CDM8 construct stained specifically with the IIIA4 antibody, thereby confirming that the antigen recognized by the IIIA4 antibody and the expressed protein product of the HEK cDNA clone were identical [9].

Chemical compound and disease context of EPHA3

  • 2. Sodium butyrate treatment increased the expression level of human (h)5-HT1B receptors in HEK 293 cells and h5-HT1D receptors in C6 glioma cells approximately 3 fold, the binding affinities of [3H]-5-HT and [3H]-alniditan were unaffected [10].
  • In the present study, HEK cells expressing the GluR6 +/- KA2 receptor subunit(s) were studied for their susceptibility to toxicity through the kainate receptor by kainate ligands [11].

Biological context of EPHA3


Anatomical context of EPHA3


Associations of EPHA3 with chemical compounds

  • Human alpha4beta2 neuronal nicotinic acetylcholine receptor in HEK 293 cells: A patch-clamp study [18].
  • However, under conditions of deoxynucleotide depletion produced by hydroxyurea treatment of HEK 293 cells, all mutants but not the wild-type virus exhibited a reduced replication phenotype similar to that observed in HCC cells [19].
  • In contrast, ouabain-inhibitable Na+ efflux in control HEK 293 cells is similarly sensitive to either 1 microM or 1 mM ouabain [20].
  • Progressive truncation and serine/threonine to alanine mutations of the PhLP(L) N terminus identified a serine/threonine cluster (Ser-18/Thr-19/Ser-20) within a small N-terminal region of PhLP(L) (amino acids 5-28) as the site in which PhLP(L) function was modified in HEK 293 cells [21].
  • We now report that in intact HEK 293 cells, PhLP(S) inhibited Gbetagamma-induced inositol phosphate generation with approximately 20-fold greater potency than PhLP(L) [21].

Other interactions of EPHA3

  • Our results indicate that AL1/LERK7 is the preferred high-affinity ligand for HEK, forming a stable 1:1 complex with a dissociation constant of 12 nM [22].
  • HEK is a member of the EPH-like receptor tyrosine kinase family, which appear to have roles in development and oncogenesis [22].
  • Ligand for EPH-related kinase (LERK) 7 is the preferred high affinity ligand for the HEK receptor [22].
  • When hepatocytic differentiation was induced in ETK-1 by 5-azacytidine, telomerase activity decreased significantly [23].

Analytical, diagnostic and therapeutic context of EPHA3

  • Southern blot analysis of DNA from LK63 suggested that the HEK gene was neither amplified nor rearranged in the LK63 tumor [9].
  • This prompted us to analyze the interactions between the HEK exodomain and fusion proteins comprising candidate LERKs and the Fc portion of human IgG1 (Fc) or a FLAGTM-peptide tag by surface plasmon resonance, size exclusion high performance liquid chromatography, sedimentation equilibrium, and transphosphorylation [22].
  • A protein purification protocol, which included HEK affinity chromatography, achieved a 1.8 X 10(6)-fold purification of an approximately 23-kDa protein from human placental conditioned medium [8].
  • Cells (HEK 293) stably transfected with two of the major brain subunits, alpha4 and beta2, were characterized electrophysiologically using the patch-clamp technique [18].
  • To determine whether a dominant negative mechanism is responsible for the autosomal dominant inheritance pattern of this disease, we studied the subcellular localization and interaction of wild type and mutant ELOVL4 in COS-7 and HEK 293T cultured cells by immunofluorescence and co-immunoprecipitation [24].


  1. Somatic mutations of GUCY2F, EPHA3, and NTRK3 in human cancers. Wood, L.D., Calhoun, E.S., Silliman, N., Ptak, J., Szabo, S., Powell, S.M., Riggins, G.J., Wang, T.L., Yan, H., Gazdar, A., Kern, S.E., Pennacchio, L., Kinzler, K.W., Vogelstein, B., Velculescu, V.E. Hum. Mutat. (2006) [Pubmed]
  2. Transcriptional analysis of the human ornithine aminotransferase promoter. Engelhardt, J.F., Steel, G., Valle, D. J. Biol. Chem. (1991) [Pubmed]
  3. GlcNAcstatin: a Picomolar, Selective O-GlcNAcase Inhibitor That Modulates Intracellular O-GlcNAcylation Levels. Dorfmueller, H.C., Borodkin, V.S., Schimpl, M., Shepherd, S.M., Shpiro, N.A., Aalten, D.M. J. Am. Chem. Soc. (2006) [Pubmed]
  4. A gene near the D3F15S2 site on 3p is expressed in normal human kidney but not or only at a severely reduced level in 11 of 15 primary renal cell carcinomas (RCC). Erlandsson, R., Bergerheim, U.S., Boldog, F., Marcsek, Z., Kunimi, K., Lin, B.Y., Ingvarsson, S., Castresana, J.S., Lee, W.H., Lee, E. Oncogene (1990) [Pubmed]
  5. Porcine endogenous retrovirus infects but does not replicate in nonhuman primate primary cells and cell lines. Ritzhaupt, A., Van Der Laan, L.J., Salomon, D.R., Wilson, C.A. J. Virol. (2002) [Pubmed]
  6. Inhibiting farnesylation of progerin prevents the characteristic nuclear blebbing of Hutchinson-Gilford progeria syndrome. Capell, B.C., Erdos, M.R., Madigan, J.P., Fiordalisi, J.J., Varga, R., Conneely, K.N., Gordon, L.B., Der, C.J., Cox, A.D., Collins, F.S. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  7. Cofactors of serine racemase that physiologically stimulate the synthesis of the N-methyl-D-aspartate (NMDA) receptor coagonist D-serine. De Miranda, J., Panizzutti, R., Foltyn, V.N., Wolosker, H. Proc. Natl. Acad. Sci. U.S.A. (2002) [Pubmed]
  8. Purification of a ligand for the EPH-like receptor HEK using a biosensor-based affinity detection approach. Lackmann, M., Bucci, T., Mann, R.J., Kravets, L.A., Viney, E., Smith, F., Moritz, R.L., Carter, W., Simpson, R.J., Nicola, N.A., Mackwell, K., Nice, E.C., Wilks, A.F., Boyd, A.W. Proc. Natl. Acad. Sci. U.S.A. (1996) [Pubmed]
  9. Molecular cloning of HEK, the gene encoding a receptor tyrosine kinase expressed by human lymphoid tumor cell lines. Wicks, I.P., Wilkinson, D., Salvaris, E., Boyd, A.W. Proc. Natl. Acad. Sci. U.S.A. (1992) [Pubmed]
  10. Agonistic properties of alniditan, sumatriptan and dihydroergotamine on human 5-HT1B and 5-HT1D receptors expressed in various mammalian cell lines. Lesage, A.S., Wouters, R., Van Gompel, P., Heylen, L., Vanhoenacker, P., Haegeman, G., Luyten, W.H., Leysen, J.E. Br. J. Pharmacol. (1998) [Pubmed]
  11. Cytotoxic effects of kainate ligands on HEK cell lines expressing recombinant kainate receptors. Carver, J.M., Mansson, P.E., Cortes-Burgos, L., Shu, J., Zhou, L.M., Howe, J.R., Giordano, T. Brain Res. (1996) [Pubmed]
  12. Distinct subdomains of the EphA3 receptor mediate ligand binding and receptor dimerization. Lackmann, M., Oates, A.C., Dottori, M., Smith, F.M., Do, C., Power, M., Kravets, L., Boyd, A.W. J. Biol. Chem. (1998) [Pubmed]
  13. Localization of a human receptor tyrosine kinase (ETK1) to chromosome region 3p11.2. Wicks, I.P., Lapsys, N.M., Baker, E., Campbell, L.J., Boyd, A.W., Sutherland, G.R. Genomics (1994) [Pubmed]
  14. Interaction between the insulin receptor and Grb14: A dynamic study in living cells using BRET. Nouaille, S., Blanquart, C., Zilberfarb, V., Boute, N., Perdereau, D., Burnol, A.F., Issad, T. Biochem. Pharmacol. (2006) [Pubmed]
  15. PCR mediated detection of a new human receptor-tyrosine-kinase, HEK 2. Böhme, B., Holtrich, U., Wolf, G., Luzius, H., Grzeschik, K.H., Strebhardt, K., Rübsamen-Waigmann, H. Oncogene (1993) [Pubmed]
  16. Endogenous channels in HEK cells and potential roles in HCN ionic current measurements. Varghese, A., Tenbroek, E.M., Coles, J., Sigg, D.C. Prog. Biophys. Mol. Biol. (2006) [Pubmed]
  17. Apoptosis induced by microinjection of cytochrome c is caspase-dependent and is inhibited by Bcl-2. Brustugun, O.T., Fladmark, K.E., Doskeland, S.O., Orrenius, S., Zhivotovsky, B. Cell Death Differ. (1998) [Pubmed]
  18. Human alpha4beta2 neuronal nicotinic acetylcholine receptor in HEK 293 cells: A patch-clamp study. Buisson, B., Gopalakrishnan, M., Arneric, S.P., Sullivan, J.P., Bertrand, D. J. Neurosci. (1996) [Pubmed]
  19. Hepatitis B virus mutants associated with 3TC and famciclovir administration are replication defective. Melegari, M., Scaglioni, P.P., Wands, J.R. Hepatology (1998) [Pubmed]
  20. ATP1AL1, a member of the non-gastric H,K-ATPase family, functions as a sodium pump. Grishin, A.V., Caplan, M.J. J. Biol. Chem. (1998) [Pubmed]
  21. Regulation of phosducin-like protein by casein kinase 2 and N-terminal splicing. Humrich, J., Bermel, C., Grubel, T., Quitterer, U., Lohse, M.J. J. Biol. Chem. (2003) [Pubmed]
  22. Ligand for EPH-related kinase (LERK) 7 is the preferred high affinity ligand for the HEK receptor. Lackmann, M., Mann, R.J., Kravets, L., Smith, F.M., Bucci, T.A., Maxwell, K.F., Howlett, G.J., Olsson, J.E., Vanden Bos, T., Cerretti, D.P., Boyd, A.W. J. Biol. Chem. (1997) [Pubmed]
  23. Telomerase activity is repressed during differentiation along the hepatocytic and biliary epithelial lineages: verification on immortal cell lines from the same origin. Fukutomi, M., Enjoji, M., Iguchi, H., Yokota, M., Iwamoto, H., Nakamuta, M., Sakai, H., Nawata, H. Cell Biochem. Funct. (2001) [Pubmed]
  24. Dominant negative mechanism underlies autosomal dominant Stargardt-like macular dystrophy linked to mutations in ELOVL4. Grayson, C., Molday, R.S. J. Biol. Chem. (2005) [Pubmed]
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