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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.
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.
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.
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.
A receptor tyrosine kinase activated by angiopoietin-1 and antagonised or weakly activated by angiopoietin-2, signalling through AKT to stabilise the endothelium.
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.
Tumour-associated overexpression: HPA finds the RNA cancer enhanced in cancer (Kidney Renal Clear Cell Carcinoma (TCGA)) and tissue enhanced in normal placenta, so the tumour and the normal tissue it comes from share the target and the medicine relies on the difference in level. HPA TEK: RNA tissue enhanced (placenta 44 nTPM); high antibody staining in 1 normal tissue. Distribution: 3 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Colorectal cancer, Hepatocellular carcinoma, Renal cell carcinoma); Open Targets associates it with 2 specific cancer types at or above 0.5 (colorectal cancer, medullary thyroid gland carcinoma). (Rule 7 of scripts/fetch-target-specificity.ts.)
Sources: Human Protein Atlas TEK tissue; Human Protein Atlas TEK pathology; Open Targets ENSG00000120156 associations
First described 1993. Earliest sequence paper UniProt cites for the protein: Ziegler S.F. et al, Oncogene, 1993, "Molecular cloning and characterization of a novel receptor protein tyrosine kinase from human placenta". Source.
A receptor tyrosine kinase activated by angiopoietin-1 and antagonised or weakly activated by angiopoietin-2, signalling through AKT to stabilise the endothelium.
RNA: tissue enhanced (placenta 44 nTPM), detected in many normal tissues.
RNA cancer enhanced: Kidney Renal Clear Cell Carcinoma 13 pTPM.
No cancer stained high; medium in carcinoid, cervical cancer, liver cancer, melanoma.
HPA TEK tissue · HPA TEK pathology · HPA protein class: CD markers, 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 (TIE2 on blood-vessel endothelium); 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:"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.
Shares Regorafenib, Renal cell carcinoma, Hepatocellular carcinoma, Colorectal cancer.
Shares Cabozantinib, Renal cell carcinoma, Hepatocellular carcinoma.
Shares Regorafenib, VEGF / VEGFR, Colorectal cancer.
Shares Cabozantinib, Renal cell carcinoma.
Shares VEGF / VEGFR, Colorectal cancer.
Shares Cabozantinib, Colorectal cancer.
Shares Cabozantinib, Renal cell carcinoma.
Shares Regorafenib, Hepatocellular carcinoma.