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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.
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).
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.
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.
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.
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.
Specificity not established: no corpus medicine is aimed at it and the catalogues give it only the role drug-target; HPA finds the RNA group enriched, which says where the protein sits but not whether the tumour differs from normal tissue. HPA EPHA1: RNA group enriched (esophagus 56 nTPM, parathyroid gland 194 nTPM); blood lineage lineage enriched (T-cells 4 nTPM); no normal tissue stained high; highest cancer staining colorectal cancer (6 of 12 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Thyroid cancer, Neuroendocrine tumours); Open Targets associates it with 1 specific cancer type at or above 0.5 (medullary thyroid gland carcinoma). (No rule of scripts/fetch-target-specificity.ts fired.)
Sources: Human Protein Atlas EPHA1 tissue; Open Targets ENSG00000146904 associations
First described 1987. Earliest sequence paper UniProt cites for the protein: Hirai et al, Science, 1987, "A novel putative tyrosine kinase receptor encoded by the eph gene". Source.
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))
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).
RNA: group enriched (esophagus 56 nTPM, parathyroid gland 194 nTPM), detected in many normal tissues. Blood: lineage enriched (T-cells 4 nTPM).
No normal tissue stained high.
Medium only: carcinoid, cervical cancer, head and neck cancer, liver 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:"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.
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.
Shares Thyroid cancer, Open Targets Platform.