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EPHA3 (Ephrin type-A receptor 3) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver and a tumour suppressor, and an approved or late-stage drug is recorded against it. Tied to Neuroendocrine tumours, Thyroid cancer, Breast cancer and 5 more.
Receptor tyrosine kinase which binds promiscuously 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 for ephrin-A ligands it binds preferentially EFNA5.
Open Targets scores its association with cancer at 0.69 (direct and indirect evidence; datatypes genetic literature 0.30, clinical 0.93, affected pathway 0.61, literature 0.96, genetic association 0.26, somatic mutation 0.47, animal model 0.39). IntOGen calls it a driver in 5 cohorts (3 activating, 2 loss-of-function), covering Invasive Breast Carcinoma, Oesophageal Adenocarcinoma, Melanoma, Prostate Adenocarcinoma, Stomach Adenocarcinoma.
In plain words · EPHA3 (Ephrin type-A receptor 3) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver and a tumour suppressor, and an approved or late-stage drug is recorded against it. Tied to Neuroendocrine tumours, Thyroid cancer, Breast cancer and 5 more.
EPHA3 (Ephrin type-A receptor 3) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, an oncogene driver and a tumour suppressor, and an approved or late-stage drug is recorded against it. Tied to Neuroendocrine tumours, Thyroid cancer, Breast cancer and 5 more.
Receptor tyrosine kinase which binds promiscuously 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 EPHA3 yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Tumour-specific alteration: the catalogues call it an oncogene driver (IntOGen cohort analysis finds it activated more often than chance) and a tumour suppressor (IntOGen finds it knocked out more often than chance), so the direction differs between cohorts but the alteration is somatic either way; what a medicine would aim at or exploit is the altered form or its loss, absent from normal cells; no corpus medicine is aimed at it yet. HPA EPHA3: RNA tissue enhanced (prostate 30 nTPM); no normal tissue stained high. Distribution: 7 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Neuroendocrine tumours, Thyroid cancer, Breast cancer (all types), Oesophageal cancer, Prostate cancer, Gastric & gastro-oesophageal junction cancer, Skin cancer (all types)); Open Targets associates it with 1 specific cancer type at or above 0.5 (medullary thyroid gland carcinoma). (Rule 6 of scripts/fetch-target-specificity.ts.)
Sources: UniProt P29320; IntOGen EPHA3; Human Protein Atlas EPHA3 tissue; Open Targets ENSG00000044524 associations
First described 1992. Earliest sequence paper UniProt cites for the protein: Wicks I.P. et al, Proc. Natl. Acad. Sci. U.S.A, 1992, "Molecular cloning of HEK, the gene encoding a receptor tyrosine kinase expressed by human lymphoid tumor cell lines". Source.
Sources: HGNC HGNC:3387 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P29320 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000044524 (association with cancer (MONDO_0004992) 0.69; per-cancer scores at or above 0.5: thyroid cancer 0.62, neuroendocrine neoplasm 0.62 (GraphQL API, CC0)); IntOGen EPHA3 (driver in 5 cohorts (Act 3, LoF 2); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Receptor tyrosine kinase which binds promiscuously 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 for ephrin-A ligands it binds preferentially EFNA5. Upon activation by EFNA5 regulates cell-cell adhesion, cytoskeletal organisation and cell migration. Also activated by EFNA1, inhibiting epithelial-to-mesenchymal transition of cardiac cells and playing a role in heart development. Involved in the retinotectal mapping of neurons. Location: Cell membrane; Secreted (UniProt). Locus 3p11.1 (HGNC).
RNA: tissue enhanced (prostate 30 nTPM), detected in many normal tissues.
No normal tissue stained high; medium in Adipose tissue, Bronchus, Caudate, Cerebral cortex, Duodenum, Gallbladder and more.
No cancer stained high; medium in breast cancer, cervical cancer, endometrial cancer, glioma.
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:"EPHA3" OR ABSTRACT:"EPHA3" OR TITLE:"EPH receptor A3" OR ABSTRACT:"EPH receptor A3" OR TITLE:"Ephrin type-A receptor 3" OR ABSTRACT:"Ephrin type-A receptor 3" OR TITLE:"HEK4" OR ABSTRACT:"HEK4" OR TITLE:"ETK1" OR ABSTRACT:"ETK1" OR TITLE:"TYRO4" OR ABSTRACT:"TYRO4") 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 EPHA3, not a curated reading list.
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Gastric & gastro-oesophageal junction cancer.
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Gastric & gastro-oesophageal junction cancer.
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Breast cancer (all types).
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Gastric & gastro-oesophageal junction cancer.
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Breast cancer (all types).
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Open Targets Platform.
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Melanoma.
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Melanoma.