EPHA3
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase which binds promiscuously membrane-bound ephrin family ligands residing on adjacent cells, leading to contact-dependent bidirectional signalling into neighboring cells.
- 3 · How drugs use it
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.
External identifiers
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)
Biology
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).
- Neuroendocrine tumours: Open Targets association 0.62 with neuroendocrine neoplasm (MONDO_0019496)
- Thyroid cancer: Open Targets association 0.62 with thyroid cancer (MONDO_0002108)
- Breast cancer: IntOGen driver in 1 cohort (BRCA)
- Oesophageal cancer: IntOGen driver in 1 cohort (ESCA)
- Prostate cancer: IntOGen driver in 1 cohort (PRAD)
- Gastric & gastro-oesophageal junction cancer: IntOGen driver in 1 cohort (STAD)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.93; IntOGen calls it an activating (Act) driver in 3 cohorts; IntOGen calls it a loss-of-function (LoF) driver in 2 cohorts. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery 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.
Similar pages
not linked directly; found by shared links- TargetNCOA2
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, Breast cancer (all types), IntOGen.
- TargetNBEA
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, Breast cancer (all types), IntOGen.
- TargetKAT6A
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, Breast cancer (all types), IntOGen.
- TargetNUMA1
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, Breast cancer (all types), IntOGen.
- TargetCDH11
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, Breast cancer (all types), IntOGen.
- TargetZNF750
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Open Targets Platform.
- TargetNUTM1
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Melanoma.
- TargetCDX2
Shares Oesophageal and junctional adenocarcinoma, Oesophageal cancer, IntOGen, Melanoma.