Vascular endothelial growth factor receptor 2 (VEGFR2) and related receptor tyrosine kinases (VEGFR2/PDGFR family)

Vascular endothelial growth factor receptor 2 (VEGFR2) is a primary receptor tyrosine kinase that mediates the effects of VEGF-A, playing a central role in angiogenesis and vascular permeability (UniProt P35968). This target entry also encompasses related members of the VEGF and PDGF receptor families, such as VEGFR1, VEGFR3, PDGFR-alpha, and PDGFR-beta, which are structurally similar and often co-targeted by multi-kinase inhibitors (StatPearls, Angiogenesis Inhibitors). These receptors are essential for the formation of new blood vessels and the maintenance of the vascular system, but their dysregulation is a hallmark of tumor growth, metastasis, and various ocular diseases (PubMed, PMID: 29158371). In oncology, drugs targeting these kinases aim to starve tumors by inhibiting the blood supply required for nutrient delivery and waste removal (NIH, National Cancer Institute). Because these receptors are also expressed in normal tissues, therapeutic intervention often leads to off-tumor effects like hypertension and proteinuria (PubMed, PMID: 24631652). Understanding the collective signaling of these families is crucial for developing effective anti-angiogenic strategies and managing the complex safety profiles of multi-targeted tyrosine kinase inhibitors.

Other names

Kinase insert domain receptorKDRFetal liver kinase 1FLK1CD309VEGF receptor familyPDGF receptor familyVascular endothelial growth factor receptor 1 (VEGFR1)Vascular endothelial growth factor receptor 3 (VEGFR3)Platelet-derived growth factor receptor alpha (PDGFRA)Platelet-derived growth factor receptor beta (PDGFRB)FLT1FLT4

Small molecule inhibition of the intracellular tyrosine kinase domain through ATP-competitive binding and monoclonal antibody-mediated blockade of the extracellular ligand-binding domain.