Ephrin type-A receptor 4
Also known as: EPHA4, HEK8, SEK, TYRO1
Function
Receptor tyrosine kinase which binds 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, it has the unique property among Eph receptors to bind and to be physiologically activated by both GPI-anchored ephrin-A and transmembrane ephrin-B ligands including EFNA1 and EFNB3. Upon activation by ephrin ligands, modulates cell morphology and integrin-dependent cell adhesion through regulation of the Rac, Rap and Rho GTPases activity. Plays an important role in the development of the nervous system controlling different steps of axonal guidance including the establishment of the corticospinal projections. May also control the segregation of motor and sensory axons during neuromuscular circuit development. In addition to its role in axonal guidance plays a role in synaptic plasticity. Activated by EFNA1 phosphorylates CDK5 at 'Tyr-15' which in turn phosphorylates NGEF regulating RHOA and dendritic spine morphogenesis. In the nervous system, also plays a role in repair after injury preventing axonal regeneration and in angiogenesis playing a role in central nervous system vascular formation. Additionally, its promiscuity makes it available to participate in a variety of cell-cell signaling regulating for instance the development of the thymic epithelium. During development of the cochlear organ of Corti, regulates pillar cell separation by forming a ternary complex with ADAM10 and CADH1 which facilitates the cleavage of CADH1 by ADAM10 and disruption of adherens junctions (By similarity). Phosphorylates CAPRIN1, promoting CAPRIN1-dependent formation of a membraneless compartment (By similarity).
Classification
- Family (Pfam)
- PF14575 EphA2_TM, PF25599 Ephrin_CRD, PF01404 Ephrin_lbd, PF00041 fn3, PF07714 PK_Tyr_Ser-Thr, PF07647 SAM_2
- InterPro
- Eph_TM, EphA4_rcpt_lig-bd, EphA4_SAM, Ephrin_rcpt_lig-bd_dom, Ephrin_rcpt_TKs, FN3_dom, FN3_sf, Galactose-bd-like_sf, Ig-like_fold, Kinase-like_dom_sf, Prot_kinase_dom, Protein_kinase_ATP_BS, SAM, SAM/pointed_sf, Ser-Thr/Tyr_kinase_cat_dom, Tyr_kinase_AS, Tyr_kinase_cat_dom, Tyr_kinase_ephrin_rcpt, Tyr_kinase_rcpt_V_CS
- Functional cluster
- Immunoglobulin-Domain Cell Adhesion Proteins
Experimental structures · PDB · 17
- 2LW8 NMR
- 2WO1 X-ray 1.85A
- 2WO2 X-ray 2.45A
- 2WO3 X-ray 2.35A
- 3CKH X-ray 2.80A
- 3GXU X-ray 2.50A
- 4BK4 X-ray 3.65A
- 4BK5 X-ray 4.00A
- 4BKA X-ray 5.30A
- 4BKF X-ray 4.65A
- 4M4P X-ray 2.08A
- 4M4R X-ray 3.13A
- … and 5 more
A predicted model is available from AlphaFold.
Gene Ontology · 71
- GO:0005912 adherens junction
- GO:0030424 axon
- GO:0043679 axon terminus
- GO:0044295 axonal growth cone
- GO:0009986 cell surface
- GO:0005737 cytoplasm
- GO:0030425 dendrite
- GO:0043198 dendritic shaft
- GO:0043197 dendritic spine
- GO:0031901 early endosome membrane
- GO:0030175 filopodium
- GO:0098978 glutamatergic synapse
- GO:0005741 mitochondrial outer membrane
- GO:0031594 neuromuscular junction
- GO:0043204 perikaryon
- GO:0005886 plasma membrane
- GO:0098839 postsynaptic density membrane
- GO:0042734 presynaptic membrane
- GO:0098685 Schaffer collateral - CA1 synapse
- GO:0001540 amyloid-beta binding
- GO:0005524 ATP binding
- GO:0097161 DH domain binding
- GO:0005003 ephrin receptor activity
- GO:0046875 ephrin receptor binding
- GO:0005004 GPI-linked ephrin receptor activity
- GO:0042802 identical protein binding
- GO:0016301 kinase activity
- GO:0042731 PH domain binding
- GO:0004713 protein tyrosine kinase activity
- GO:1990782 protein tyrosine kinase binding
- GO:0005005 transmembrane-ephrin receptor activity
- GO:0034332 adherens junction organization
- GO:0007411 axon guidance
- GO:0007155 cell adhesion
- GO:1904646 cellular response to amyloid-beta
- GO:0090102 cochlea development
- GO:0021957 corticospinal tract morphogenesis
- GO:0048013 ephrin receptor signaling pathway
- GO:0097156 fasciculation of motor neuron axon
- GO:0097155 fasciculation of sensory neuron axon
- GO:0008347 glial cell migration
- GO:0008045 motor neuron axon guidance
- GO:0048681 negative regulation of axon regeneration
- GO:0007162 negative regulation of cell adhesion
- GO:0030336 negative regulation of cell migration
- GO:1900038 negative regulation of cellular response to hypoxia
- GO:0010719 negative regulation of epithelial to mesenchymal transition
- GO:0070373 negative regulation of ERK1 and ERK2 cascade
- GO:1900272 negative regulation of long-term synaptic potentiation
- GO:0010977 negative regulation of neuron projection development
- GO:1903051 negative regulation of proteolysis involved in protein catabolic process
- GO:0017148 negative regulation of translation
- GO:0106030 neuron projection fasciculation
- GO:0097485 neuron projection guidance
- GO:1902993 positive regulation of amyloid precursor protein catabolic process
- GO:1902004 positive regulation of amyloid-beta formation
- GO:0045785 positive regulation of cell adhesion
- GO:0030335 positive regulation of cell migration
- GO:0008284 positive regulation of cell population proliferation
- GO:0050775 positive regulation of dendrite morphogenesis
- GO:1902533 positive regulation of intracellular signal transduction
- GO:0046330 positive regulation of JNK cascade
- GO:1904999 positive regulation of leukocyte adhesion to arterial endothelial cell
- GO:0050821 protein stabilization
- GO:0048710 regulation of astrocyte differentiation
- GO:0050770 regulation of axonogenesis
- GO:0061001 regulation of dendritic spine morphogenesis
- GO:0043087 regulation of GTPase activity
- GO:1905244 regulation of modification of synaptic structure
- GO:1905806 regulation of synapse pruning
- GO:0098883 synapse pruning
Drugs targeting this protein · 1
- VANDETANIB inhibitor
Related proteins · sequence + function similarity
- Ephrin type-A receptor 4 1.00
- Ephrin type-A receptor 4 0.99
- Ephrin type-A receptor 4-A 0.98
- Ephrin type-A receptor 4-B 0.98
- Ephrin type-A receptor 7 0.96
- Ephrin type-B receptor 2 0.96
- Ephrin type-B receptor 2 0.95
- Ephrin type-B receptor 2 0.95
- Ephrin type-B receptor 2 0.95
- Ephrin type-A receptor 3 0.95
- Ephrin type-B receptor 1 0.95
- Ephrin type-B receptor 1 0.95
Co-cited proteins · studied together in the literature
- Ephrin-B2 2 shared papers
- Ephrin-A2 1 shared papers
- Ephrin type-A receptor 7 2 shared papers
- Ephrin type-A receptor 5 2 shared papers
- Signal-induced proliferation-associated 1-like protein 1 1 shared papers
- Signal-induced proliferation-associated 1-like protein 1 1 shared papers
- Ephrin type-B receptor 2 2 shared papers
- Ephrin type-A receptor 4 1 shared papers
- Ephrin type-A receptor 4 2 shared papers
- Signal-induced proliferation-associated 1-like protein 1 1 shared papers
- Cyclin-dependent kinase 5 activator 1 1 shared papers
- Cyclin-dependent kinase 5 activator 1 1 shared papers
Literature · 12 cited papers
- Structural characterization of the EphA4-Ephrin-B2 complex reveals new features enabling Eph-ephrin binding promiscuity. J. Biol. Chem. · 2010
- Structural plasticity of EPH receptor A4 facilitates cross-class ephrin signaling. Structure · 2009
- Large-scale proteomics analysis of the human kinome. Mol. Cell. Proteomics · 2009
- Crystal structure and NMR binding reveal that two small molecule antagonists target the high affinity ephrin-binding channel of the EphA4 receptor. J. Biol. Chem. · 2008
- The EphA4 receptor regulates neuronal morphology through SPAR-mediated inactivation of Rap GTPases. J. Neurosci. · 2007
- Patterns of somatic mutation in human cancer genomes. Nature · 2007
- Cdk5 regulates EphA4-mediated dendritic spine retraction through an ephexin1-dependent mechanism. Nat. Neurosci. · 2007
- Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature · 2005
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
- Unified nomenclature for Eph family receptors and their ligands, the ephrins. Cell · 1997
- cDNA cloning and tissue distribution of five human EPH-like receptor protein-tyrosine kinases. Oncogene · 1995