Vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) family (VEGFR and PDGFR)

The Vascular Endothelial Growth Factor Receptor (VEGFR) and Platelet-Derived Growth Factor Receptor (PDGFR) families are critical subfamilies of receptor tyrosine kinases (RTKs) that regulate vascular development and mesenchymal cell function. The VEGFR family, including VEGFR-1, -2, and -3, primarily drives angiogenesis and lymphangiogenesis, which are essential for supplying nutrients to tumors and facilitating metastasis (Ferrara, 2004, Nature). The PDGFR family, consisting of PDGFR-alpha and -beta, regulates the recruitment of pericytes and fibroblasts that stabilize blood vessels and contribute to the high interstitial fluid pressure within the tumor microenvironment (Andrae et al., 2008, Genes & Development). Because these families work synergistically to support tumor growth and survival, they are frequently targeted simultaneously by multi-kinase inhibitors like sunitinib and pazopanib. Beyond oncology, these receptors play significant roles in ophthalmic diseases like wet age-related macular degeneration and fibrotic conditions such as idiopathic pulmonary fibrosis (StatPearls, 2023). Therapeutic modulation of these pathways requires careful management of systemic side effects, most notably hypertension and vascular complications, due to their fundamental roles in normal vascular homeostasis (PubMed: 21358671).

Other names

VEGF receptorsPDGF receptorsClass III and IV Receptor Tyrosine KinasesRTK Class III/IV

Inhibition of the intracellular tyrosine kinase domain by competing with adenosine triphosphate (ATP) for the binding site, which prevents receptor autophosphorylation and blocks downstream signaling pathways such as Ras/MAPK, PI3K/Akt, and PLC-gamma (StatPearls, 2023; PubMed: 12675858).