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EPHA4 (Ephrin type-A receptor 4) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Thyroid cancer and Neuroendocrine tumours.
Receptor tyrosine kinase which binds membrane-bound ephrin family ligands residing on adjacent cells, leading to contact-dependent bidirectional signalling into neighboring cells. The signalling pathway downstream of the receptor is referred to as forward signalling while the signalling pathway downstream of the ephrin ligand is referred to as reverse signalling. 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.
Open Targets scores its association with cancer at 0.66 (direct and indirect evidence; datatypes literature 0.94, animal model 0.66, genetic association 0.39, clinical 0.93).
In plain words · EPHA4 (Ephrin type-A receptor 4) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Thyroid cancer and Neuroendocrine tumours.
EPHA4 (Ephrin type-A receptor 4) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Thyroid cancer and Neuroendocrine tumours.
Receptor tyrosine kinase which binds membrane-bound ephrin family ligands residing on adjacent cells, leading to contact-dependent bidirectional signalling into neighboring cells.
No product in this corpus aims at EPHA4 yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Specificity not established: no corpus medicine is aimed at it and the catalogues give it only the role drug-target; HPA finds the RNA tissue enhanced, which says where the protein sits but not whether the tumour differs from normal tissue. HPA EPHA4: RNA tissue enhanced (brain 24 nTPM); high antibody staining in 3 normal tissues; highest cancer staining thyroid cancer (4 of 4 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Thyroid cancer, Neuroendocrine tumours); Open Targets associates it with 1 specific cancer type at or above 0.5 (medullary thyroid gland carcinoma). (No rule of scripts/fetch-target-specificity.ts fired.)
Sources: Human Protein Atlas EPHA4 tissue; Open Targets ENSG00000116106 associations
First described 1995. Earliest sequence paper UniProt cites for the protein: Fox G.M. et al, Oncogene, 1995, "cDNA cloning and tissue distribution of five human EPH-like receptor protein-tyrosine kinases". Source.
Sources: HGNC HGNC:3388 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P54764 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000116106 (association with cancer (MONDO_0004992) 0.66; per-cancer scores at or above 0.5: thyroid cancer 0.56, neuroendocrine neoplasm 0.55 (GraphQL API, CC0))
Receptor tyrosine kinase which binds membrane-bound ephrin family ligands residing on adjacent cells, leading to contact-dependent bidirectional signalling into neighboring cells. The signalling pathway downstream of the receptor is referred to as forward signalling while the signalling pathway downstream of the ephrin ligand is referred to as reverse signalling. 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. Location: Cell membrane; Cell projection, axon; Cell projection, dendrite; Postsynaptic density membrane (UniProt). Locus 2q36.1 (HGNC).
RNA: tissue enhanced (brain 24 nTPM), detected in many normal tissues.
Medium: Bone marrow, Colon, Kidney, Nasopharynx, Skin, Spleen, Testis, Thyroid gland.
RNA cancer enhanced: Thyroid Carcinoma 20 pTPM.
Medium only: breast cancer, carcinoid, endometrial cancer, pancreatic cancer.
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query for this target: (TITLE:"EPHA4" OR ABSTRACT:"EPHA4" OR TITLE:"EPH receptor A4" OR ABSTRACT:"EPH receptor A4" OR TITLE:"Ephrin type-A receptor 4" OR ABSTRACT:"Ephrin type-A receptor 4" OR TITLE:"Hek8" OR ABSTRACT:"Hek8" OR TITLE:"TYRO1" OR ABSTRACT:"TYRO1") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about EPHA4, not a curated reading list.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Open Targets Platform.