Vascular endothelial growth factor receptor 1 (VEGFR-1) (VEGFR-1)

Vascular endothelial growth factor receptor 1 (VEGFR-1), also known as Fms-like tyrosine kinase 1 (FLT-1), is a cell-surface receptor tyrosine kinase that plays a critical role in the regulation of angiogenesis and vasculogenesis [UniProt: P17948]. It binds with high affinity to VEGF-A, VEGF-B, and placental growth factor (PlGF), often acting as a "decoy" receptor that sequesters VEGF-A to modulate its interaction with VEGFR-2 [PubMed: 11085981]. Beyond its decoy function, VEGFR-1 signaling is involved in the recruitment of bone marrow-derived cells and the promotion of inflammatory processes [PubMed: 16461337]. In clinical oncology, VEGFR-1 is a major target for multi-kinase inhibitors like sunitinib and sorafenib, which block its intracellular kinase activity to inhibit tumor blood vessel growth [PubChem: CID 5329102]. Additionally, a soluble form of the receptor (sFlt-1) is a significant biomarker in preeclampsia, where elevated levels contribute to endothelial dysfunction [NIH: NBK532910]. Therapeutic targeting of VEGFR-1 is essential for treating various cancers and neovascular eye diseases, though it is associated with side effects such as hypertension and proteinuria [PubMed: 20634430]. The receptor's complex role as both a signaling molecule and a negative regulator makes it a unique focus in vascular biology and drug development.

Other names

Fms-like tyrosine kinase 1FLT-1Tyrosine-protein kinase FRTVascular endothelial growth factor receptor 1

Inhibition of the intracellular tyrosine kinase domain to block downstream signaling pathways and sequestration of VEGF ligands to prevent receptor activation [PubMed: 11085981, PubChem: CID 5329102].