{"entity":{"id":"tie2","kind":"target","name":"TIE2 receptor (TEK)","aka":[],"tldr":"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.","summary":"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.","asOf":"2026-09-04","wikipedia":"https://en.wikipedia.org/wiki/TEK_tyrosine_kinase","links":[{"label":"UniProt Q02763: TEK","url":"https://www.uniprot.org/uniprotkb/Q02763/entry"},{"label":"HGNC:11724 TEK","url":"https://www.genenames.org/data/gene-symbol-report/#!/hgnc_id/HGNC:11724"},{"label":"ChEMBL target CHEMBL4128","url":"https://www.ebi.ac.uk/chembl/explore/target/CHEMBL4128"}],"tags":[],"related":["vegf"],"cancers":["colorectal","hcc","rcc"],"sections":[],"technologies":[],"targets":[],"drugs":["regorafenib","cabozantinib"],"companies":[],"institutions":[],"pathways":[],"terms":["angiogenesis"],"trials":[],"people":[],"bottlenecks":[],"keyPapers":[],"journals":[],"dependsOn":[],"notes":[],"symbol":"TEK","role":[],"sources":[],"specificity":"tumour-associated","distribution":"few-types","specificityNote":"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.)","specificitySources":[{"label":"Human Protein Atlas TEK tissue","url":"https://www.proteinatlas.org/ENSG00000120156-TEK/tissue","note":"RNA tissue and blood lineage specificity, normal tissue antibody staining (version 25.1, CC BY-SA 3.0)"},{"label":"Human Protein Atlas TEK pathology","url":"https://www.proteinatlas.org/ENSG00000120156-TEK/pathology","note":"patients per staining level per cancer type (version 25.1, CC BY-SA 3.0)"},{"label":"Open Targets ENSG00000120156 associations","url":"https://platform.opentargets.org/target/ENSG00000120156/associations","note":"cancer associations at or above 0.5 (CC0)"}],"hgnc":"HGNC:11724","ensembl":"ENSG00000120156","uniprot":"Q02763","entrez":"7010","firstDescribed":1993,"firstDescribedBasis":"sequence","firstDescribedNote":"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\".","firstDescribedSource":"https://pubmed.ncbi.nlm.nih.gov/8382358/","biology":"A receptor tyrosine kinase activated by angiopoietin-1 and antagonised or weakly activated by angiopoietin-2, signalling through AKT to stabilise the endothelium.","whereFound":["Tumour and normal endothelium","TIE2-expressing monocytes and macrophages"],"targetClass":"kinase","prevalence":[{"cancerId":"metastatic-cancer","pct":"all","measure":"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."}]},"route":"/targets/tie2/","neighbours":{"target":[{"id":"vegf","kind":"target","name":"VEGF / VEGFR","route":"/targets/vegf/"}],"cancer":[{"id":"colorectal","kind":"cancer","name":"Colorectal cancer","route":"/cancers/colorectal/"},{"id":"hcc","kind":"cancer","name":"Hepatocellular carcinoma","route":"/cancers/hcc/"},{"id":"rcc","kind":"cancer","name":"Renal cell carcinoma","route":"/cancers/rcc/"}],"drug":[{"id":"cabozantinib","kind":"drug","name":"Cabozantinib","route":"/drugs/cabozantinib/"},{"id":"regorafenib","kind":"drug","name":"Regorafenib","route":"/drugs/regorafenib/"}],"term":[{"id":"angiogenesis","kind":"term","name":"Angiogenesis","route":"/terms/angiogenesis/"}]}}