TIE2 receptor (TEK)
TIE2 is the angiopoietin receptor that keeps blood vessels stable; regorafenib and cabozantinib block it as part of their attack on the tumour's blood supply.
Overview
TEK (TIE2) is the receptor for angiopoietins 1 and 2 on endothelial cells and a subset of macrophages, controlling vessel maturation and remodelling. Regorafenib and cabozantinib inhibit TIE2 alongside VEGF receptors, and the angiopoietin-2 antibody trebananib was tested in ovarian cancer without approval. TIE2-expressing macrophages are a source of resistance to anti-VEGF therapy.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · TIE2 is the angiopoietin receptor that keeps blood vessels stable; regorafenib and cabozantinib block it as part of their attack on the tumour's blood supply.
- 1 · What it is
TIE2 is the angiopoietin receptor that keeps blood vessels stable; regorafenib and cabozantinib block it as part of their attack on the tumour's blood supply.
- 2 · What goes wrong in cancer
A receptor tyrosine kinase activated by angiopoietin-1 and antagonised or weakly activated by angiopoietin-2, signalling through AKT to stabilise the endothelium.
- 3 · How drugs use it
No product in this corpus aims at TIE2 receptor (TEK) 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 activated by angiopoietin-1 and antagonised or weakly activated by angiopoietin-2, signalling through AKT to stabilise the endothelium.
- Tumour and normal endothelium
- TIE2-expressing monocytes and macrophages
Latest papers
topQuery for this target: (TITLE:"TIE2 receptor" OR ABSTRACT:"TIE2 receptor" OR TITLE:"TEK" OR ABSTRACT:"TEK") 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 TIE2 receptor (TEK), not a curated reading list.
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