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Vascular endothelial growth factor receptor 1 (VEGFR1/FLT1) and vascular endothelial growth factor receptor 3 (VEGFR3/FLT4) are cell surface receptor tyrosine kinases involved in the mediation of signal transduction triggered by their ligands, members of the VEGF family. VEGFR1 binds VEGF-A, VEGF-B, and placental growth factor (PIGF) and classically functions as both a decoy receptor (regulating available VEGF-A to limit angiogenic signaling) and a signaling receptor modulating angiogenesis, vessel maintenance, and immune cell function. VEGFR3 is the main receptor for VEGF-C and VEGF-D and is crucial for lymphangiogenesis and lymphatic vessel maintenance, as well as in pathological conditions such as tumor lymphangiogenesis, lymphedema, and cancer metastasis. Both play partially redundant roles in maintaining vascular and lymphatic systems and have become important therapeutic targets in cancer and diseases of abnormal vessel growth or function.
Inhibition of ligand binding (e.g., monoclonal antibodies to VEGF ligands); Inhibition of kinase activity (small molecule inhibitors); Blocking signal transduction through VEGFR dimerization and phosphorylation.
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