EPHA1
EPHA1 (Ephrin type-A receptor 1) 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.
Overview
Receptor tyrosine kinase which binds promiscuously membrane-bound 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. Binds with a low affinity EFNA3 and EFNA4 and with a high affinity to EFNA1 which most probably constitutes its cognate/functional ligand.
Open Targets scores its association with cancer at 0.60 (direct and indirect evidence; datatypes literature 0.93, animal model 0.43, genetic association 0.00, clinical 0.93).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · EPHA1 (Ephrin type-A receptor 1) 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.
- 1 · What it is
EPHA1 (Ephrin type-A receptor 1) 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.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase which binds promiscuously membrane-bound 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 EPHA1 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:3385 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P21709 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000146904 (association with cancer (MONDO_0004992) 0.60; per-cancer scores at or above 0.5: thyroid cancer 0.56, neuroendocrine neoplasm 0.55 (GraphQL API, CC0))
Biology
Receptor tyrosine kinase which binds promiscuously membrane-bound 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. Binds with a low affinity EFNA3 and EFNA4 and with a high affinity to EFNA1 which most probably constitutes its cognate/functional ligand. Upon activation by EFNA1 induces cell attachment to the extracellular matrix inhibiting cell spreading and motility through regulation of ILK and downstream RHOA and RAC. Also plays a role in angiogenesis and regulates cell proliferation. May play a role in apoptosis. Location: Cell membrane (UniProt). Locus 7q34-q35 (HGNC).
- Thyroid cancer: Open Targets association 0.56 with thyroid cancer (MONDO_0002108)
- Neuroendocrine tumours: Open Targets association 0.55 with neuroendocrine neoplasm (MONDO_0019496)
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. 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:"EPHA1" OR ABSTRACT:"EPHA1" OR TITLE:"EPH receptor A1" OR ABSTRACT:"EPH receptor A1" OR TITLE:"Ephrin type-A receptor 1" OR ABSTRACT:"Ephrin type-A receptor 1" OR TITLE:"EPHT1" OR ABSTRACT:"EPHT1") 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 EPHA1, not a curated reading list.
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