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

VEGFRs and PDGFRs are families of receptor tyrosine kinases located on the cell surface. VEGFRs are primarily expressed on endothelial cells, where they are activated by vascular endothelial growth factor (VEGF) ligands and mediate angiogenesis, vascular permeability, and cell survival signal transduction. PDGFRs are activated by platelet-derived growth factors, controlling cell proliferation and migration, being especially critical for vascular smooth muscle cells and fibroblasts. Both families share structural features including extracellular ligand-binding immunoglobulin-like domains, a transmembrane region, and a cytoplasmic split tyrosine kinase domain. Therapeutic targeting of VEGFR and PDGFR has led to the development of many clinically approved anti-angiogenic drugs, particularly in oncology, but these treatments are associated with significant safety challenges due to their role in normal vascular physiology.

Other names

KDRFlk-1Flt-1VEGFR-1VEGFR-2VEGFR-3PDGFR-alphaPDGFR-beta

Inhibition of receptor tyrosine kinase activity, blocking ATP binding to the kinase domain and preventing downstream signaling; Anti-angiogenesis effect, reducing new blood vessel formation critical for tumor growth; Reduction of endothelial cell proliferation and migration; Suppression of cell survival signaling