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EphA2 is a cell-guidance receptor that many solid tumours overexpress; dasatinib and regorafenib block it among their many kinase targets, and it is being tested as an antibody-drug conjugate and CAR-T target.
Ephrin type-A receptor 2 helps cells read their neighbours' positions during development and is overexpressed in glioblastoma, ovarian, breast, lung and pancreatic cancers, where ligand-independent signalling promotes invasion. Dasatinib and regorafenib inhibit it as secondary targets. Antibody-drug conjugates and CAR-T cells against EphA2 have reached early trials, notably in glioblastoma.
In plain words · EphA2 is a cell-guidance receptor that many solid tumours overexpress; dasatinib and regorafenib block it among their many kinase targets, and it is being tested as an antibody-drug conjugate and CAR-T target.
EphA2 is a cell-guidance receptor that many solid tumours overexpress; dasatinib and regorafenib block it among their many kinase targets, and it is being tested as an antibody-drug conjugate and CAR-T target.
A receptor tyrosine kinase for ephrin-A ligands; ligand binding suppresses growth signalling, while unliganded EphA2 phosphorylated by AKT drives motility.
No product in this corpus aims at EphA2 receptor yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
Tumour-associated overexpression: HPA finds the RNA tissue enhanced in normal esophagus, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA EPHA2: RNA tissue enhanced (esophagus 143 nTPM); blood lineage lineage enriched (dendritic cells 9 nTPM); no normal tissue stained high. Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Brain and spinal cord tumours (all types), Ovarian cancer); Open Targets associates it with 4 specific cancer types at or above 0.5 (colorectal cancer, chronic myeloid leukemia, acute lymphoblastic leukemia, medullary thyroid gland carcinoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas EPHA2 tissue; Human Protein Atlas EPHA2 pathology; Open Targets ENSG00000142627 associations
First described 1990. Earliest sequence paper UniProt cites for the protein: Lindberg R.A. et al, Mol. Cell. Biol, 1990, "cDNA cloning and characterization of eck, an epithelial cell receptor protein-tyrosine kinase in the eph/elk family of protein kinases". Source.
A receptor tyrosine kinase for ephrin-A ligands; ligand binding suppresses growth signalling, while unliganded EphA2 phosphorylated by AKT drives motility.
RNA: tissue enhanced (esophagus 143 nTPM), detected in many normal tissues. Blood: lineage enriched (dendritic cells 9 nTPM).
No normal tissue stained high.
No cancer sample stained medium or high.
HPA EPHA2 tissue · HPA EPHA2 pathology · HPA protein class: FDA approved drug targets
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.
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Metastatic cancer | all% | Signalling protein present in most cells (EphA2 receptor, over-expressed in many solid tumours without a selecting mutation); drugs act on the pathway rather than on a mutation that selects patients, so no prevalence applies. |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Query for this target: (TITLE:"EphA2 receptor" OR ABSTRACT:"EphA2 receptor" OR TITLE:"EPHA2" OR ABSTRACT:"EPHA2") 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 EphA2 receptor, not a curated reading list.
Shares Dasatinib, Glioma & glioblastoma.
Shares Regorafenib, Glioma & glioblastoma.
Shares Regorafenib, Glioma & glioblastoma, Ovarian cancer.
Shares Dasatinib, Regorafenib.