EPHA8
EPHA8 (Ephrin type-A receptor 8) 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 Neuroendocrine tumours and Thyroid cancer.
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. The GPI-anchored ephrin-A EFNA2, EFNA3, and EFNA5 are able to activate EPHA8 through phosphorylation.
Open Targets scores its association with cancer at 0.59 (direct and indirect evidence; datatypes literature 0.62, 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 · EPHA8 (Ephrin type-A receptor 8) 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 Neuroendocrine tumours and Thyroid cancer.
- 1 · What it is
EPHA8 (Ephrin type-A receptor 8) 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 Neuroendocrine tumours and Thyroid cancer.
- 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 EPHA8 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:3391 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P29322 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000070886 (association with cancer (MONDO_0004992) 0.59; per-cancer scores at or above 0.5: thyroid cancer 0.56, neuroendocrine neoplasm 0.62 (GraphQL API, CC0))
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. The GPI-anchored ephrin-A EFNA2, EFNA3, and EFNA5 are able to activate EPHA8 through phosphorylation. With EFNA5 may regulate integrin-mediated cell adhesion and migration on fibronectin substrate but also neurite outgrowth. During development of the nervous system also plays a role in axon guidance. Downstream effectors of the EPHA8 signalling pathway include FYN which promotes cell adhesion upon activation by EPHA8 and the MAP kinases in the stimulation of neurite outgrowth. Location: Cell membrane; Cell projection; Early endosome membrane (UniProt). Locus 1p36.12 (HGNC).
- Neuroendocrine tumours: Open Targets association 0.62 with neuroendocrine neoplasm (MONDO_0019496)
- Thyroid cancer: Open Targets association 0.56 with thyroid cancer (MONDO_0002108)
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:"EPHA8" OR ABSTRACT:"EPHA8" OR TITLE:"EPH receptor A8" OR ABSTRACT:"EPH receptor A8" OR TITLE:"Ephrin type-A receptor 8" OR ABSTRACT:"Ephrin type-A receptor 8" OR TITLE:"Hek3" OR ABSTRACT:"Hek3") 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 EPHA8, not a curated reading list.
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