EPHB4
EPHB4 (Ephrin type-B receptor 4) 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 a biomarker, and an approved or late-stage drug is recorded against it. Tied to Colorectal cancer, Thyroid cancer and Neuroendocrine tumours.
Overview
Receptor tyrosine kinase which binds promiscuously to transmembrane ephrin-B 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. Together with its cognate ligand/functional ligand EFNB2, it is involved in the regulation of cell adhesion and migration, and plays a central role in heart morphogenesis, angiogenesis and blood vessel remodeling and permeability.
CIViC holds 1 clinical evidence item and 0 assertions across 1 variant, naming Bevacizumab. Open Targets scores its association with cancer at 0.61 (direct and indirect evidence; datatypes literature 0.99, genetic association 0.18, clinical 0.94).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · EPHB4 (Ephrin type-B receptor 4) 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 a biomarker, and an approved or late-stage drug is recorded against it. Tied to Colorectal cancer, Thyroid cancer and Neuroendocrine tumours.
- 1 · What it is
EPHB4 (Ephrin type-B receptor 4) 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 a biomarker, and an approved or late-stage drug is recorded against it. Tied to Colorectal cancer, Thyroid cancer and Neuroendocrine tumours.
- 2 · What goes wrong in cancer
Receptor tyrosine kinase which binds promiscuously to transmembrane ephrin-B 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 EPHB4 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:3395 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P54760 (protein name, function text, keywords and locations (REST API)); CIViC gene EPHB4 (1 evidence items, 0 assertions, 1 variants; diseases: Colorectal Cancer (GraphQL API, CC0)); Open Targets ENSG00000196411 (association with cancer (MONDO_0004992) 0.61; per-cancer scores at or above 0.5: thyroid cancer 0.57, neuroendocrine neoplasm 0.56 (GraphQL API, CC0))
Biology
Receptor tyrosine kinase which binds promiscuously to transmembrane ephrin-B 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. Together with its cognate ligand/functional ligand EFNB2, it is involved in the regulation of cell adhesion and migration, and plays a central role in heart morphogenesis, angiogenesis and blood vessel remodeling and permeability. EPHB4-mediated forward signalling controls cellular repulsion and segregation from EFNB2-expressing cells. Phosphorylates inactive tyrosine-protein kinase EPHB6 which promotes interaction of EPHB6 with SH2 domains, allowing it to recruit SH2 domain-containing signalling adapters. Location: Cell membrane (UniProt). Locus 7q22.1 (HGNC).
- Colorectal cancer: CIViC evidence names this disease
- Thyroid cancer: Open Targets association 0.57 with thyroid cancer (MONDO_0002108)
- Neuroendocrine tumours: Open Targets association 0.56 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 0.94; CIViC holds 1 clinical evidence items on its variants. 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:"EPHB4" OR ABSTRACT:"EPHB4" OR TITLE:"EPH receptor B4" OR ABSTRACT:"EPH receptor B4" OR TITLE:"Ephrin type-B receptor 4" OR ABSTRACT:"Ephrin type-B receptor 4" OR TITLE:"Tyro11" OR ABSTRACT:"Tyro11") 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 EPHB4, not a curated reading list.
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