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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.
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).
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.
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.
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.
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.
Broadly expressed or essential: HPA finds the RNA at low tissue specificity; a medicine acting on the wild-type protein would expose normal tissue too. HPA EPHB4: RNA low tissue specificity; no normal tissue stained high; highest cancer staining colorectal cancer (4 of 12 high). Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Colorectal cancer, Thyroid cancer, Neuroendocrine tumours); Open Targets associates it with 2 specific cancer types at or above 0.5 (medullary thyroid gland carcinoma, vein of Galen aneurysm). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas EPHB4 tissue; Open Targets ENSG00000196411 associations
First described 1994. Earliest sequence paper UniProt cites for the protein: Bennett B.D. et al, J. Biol. Chem, 1994, "Cloning and characterization of HTK, a novel transmembrane tyrosine kinase of the EPH subfamily". Source.
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))
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).
RNA: low tissue specificity, detected in many normal tissues.
No normal tissue stained high.
Medium only: breast cancer, carcinoid, cervical cancer, head and neck cancer.
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query 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.
Shares Thyroid cancer, Neuroendocrine tumours, CIViC, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.
Shares Thyroid cancer, Neuroendocrine tumours, Open Targets Platform.