Tyrosine-protein kinase receptor Tie-1 (TIE1)

Tyrosine-protein kinase receptor Tie-1 (TIE1) is a cell-surface receptor tyrosine kinase primarily expressed in endothelial cells and hematopoietic progenitor cells (UniProt, Wikipedia). It plays a fundamental role in vascular development, angiogenesis, and the maintenance of blood vessel integrity by modulating the angiopoietin-Tie2 signaling axis (PubMed, NCBI). Although TIE1 was long considered an orphan receptor, it is now known to interact with Tie2 to regulate endothelial cell survival and inflammatory responses, often acting as a context-dependent regulator of vascular stability (PMC, JCI). In disease states, TIE1 is frequently upregulated in tumor vasculature, where it promotes tumor growth and metastasis, and it is also implicated in the progression of atherosclerosis and lymphatic disorders like lymphedema (PubMed, GeneCards). Therapeutic strategies targeting TIE1 include the development of function-blocking antibodies, such as AB-Tie1-39, and small-molecule tyrosine kinase inhibitors aimed at disrupting its role in pathological angiogenesis and inflammation (PMC, IUPHAR). While TIE1 inhibition shows promise for treating metastatic cancers and cardiovascular diseases, potential safety concerns include impaired vascular integrity and lymphatic dysfunction (PubMed, NIH).

Other names

Tyrosine kinase with immunoglobulin-like and EGF-like domains 1TIE1JTK14TIELMPHM11Tyrosine kinase receptor 1

Inhibition of receptor tyrosine kinase activity, blocking of Tie1-Tie2 interaction, and modulation of angiopoietin-Tie2 signaling to stabilize or normalize vasculature (PubMed, PMC) [2, 3, 8].