EphA2 receptor
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.
Overview
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.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
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.
- 1 · What it is
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.
- 2 · What goes wrong in cancer
A receptor tyrosine kinase for ephrin-A ligands; ligand binding suppresses growth signalling, while unliganded EphA2 phosphorylated by AKT drives motility.
- 3 · How drugs use it
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.
External identifiers
Biology
A receptor tyrosine kinase for ephrin-A ligands; ligand binding suppresses growth signalling, while unliganded EphA2 phosphorylated by AKT drives motility.
- Glioblastoma, ovarian, breast, lung and pancreatic cancers (overexpressed)
- Low in normal adult epithelium
Latest papers
topQuery 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.
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