EPHA7
EPHA7 (Ephrin type-A receptor 7) 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 Thyroid cancer, Neuroendocrine tumours, Colorectal cancer and 2 more.
Overview
Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A 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. Among GPI-anchored ephrin-A ligands, EFNA5 is a cognate/functional ligand for EPHA7 and their interaction regulates brain development modulating cell-cell adhesion and repulsion.
Open Targets scores its association with cancer at 0.70 (direct and indirect evidence; datatypes literature 0.94, genetic association 0.28, somatic mutation 0.50, clinical 0.93). IntOGen calls it a driver in 3 cohorts (1 activating, 2 loss-of-function), covering Colorectal Adenocarcinoma, Hepatocellular Carcinoma, Lung 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 · EPHA7 (Ephrin type-A receptor 7) 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 Thyroid cancer, Neuroendocrine tumours, Colorectal cancer and 2 more.
- 1 · What it is
EPHA7 (Ephrin type-A receptor 7) 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 Thyroid cancer, Neuroendocrine tumours, Colorectal cancer and 2 more.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A 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 EPHA7 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:3390 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt Q15375 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000135333 (association with cancer (MONDO_0004992) 0.70; per-cancer scores at or above 0.5: thyroid cancer 0.62, neuroendocrine neoplasm 0.61 (GraphQL API, CC0)); IntOGen EPHA7 (driver in 3 cohorts (Act 1, LoF 2); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
Biology
Receptor tyrosine kinase which binds promiscuously GPI-anchored ephrin-A 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. Among GPI-anchored ephrin-A ligands, EFNA5 is a cognate/functional ligand for EPHA7 and their interaction regulates brain development modulating cell-cell adhesion and repulsion. Has a repellent activity on axons and is for instance involved in the guidance of corticothalamic axons and in the proper topographic mapping of retinal axons to the colliculus. May also regulate brain development through a caspase(CASP3)-dependent proapoptotic activity. Forward signalling may result in activation of components of the ERK signalling pathway including MAP2K1, MAP2K2, MAPK1 and MAPK3 which are phosphorylated upon activation of EPHA7. Location: Cell membrane (UniProt). Locus 6q16.1 (HGNC).
- Thyroid cancer: Open Targets association 0.62 with thyroid cancer (MONDO_0002108)
- Neuroendocrine tumours: Open Targets association 0.61 with neuroendocrine neoplasm (MONDO_0019496)
- Colorectal cancer: IntOGen driver in 1 cohort (COADREAD)
- Hepatocellular carcinoma: IntOGen driver in 1 cohort (HCC)
- Non-small-cell lung cancer: IntOGen driver in 1 cohort (LUAD)
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 1 cohort; 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:"EPHA7" OR ABSTRACT:"EPHA7" OR TITLE:"EPH receptor A7" OR ABSTRACT:"EPH receptor A7" OR TITLE:"Ephrin type-A receptor 7" OR ABSTRACT:"Ephrin type-A receptor 7" OR TITLE:"Hek11" OR ABSTRACT:"Hek11") 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 EPHA7, not a curated reading list.
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