VEGFR1, VEGFR3, RET

Vascular endothelial growth factor receptor 1 (VEGFR1), Vascular endothelial growth factor receptor 3 (VEGFR3), and RET proto-oncogene (RET) are single-pass transmembrane receptor tyrosine kinases that mediate critical biological processes including angiogenesis, lymphangiogenesis, cell proliferation, and survival. VEGFR1 primarily regulates blood vessel formation by acting as both a signaling and a decoy receptor for VEGF-A, while VEGFR3 drives lymphatic vessel formation by binding VEGF-C and VEGF-D. RET is a multifunctional proto-oncogene receptor implicated in development of neural crest-derived tissues, as well as several forms of cancer due to oncogenic mutation or rearrangement. Inhibitors that target these receptors are important components of current therapeutic strategies for cancer and vascular diseases, but are often limited by adverse effects related to the broad role of RTKs in physiology[2][3][4][5][6].

Other names

Flt-1fms-like tyrosine kinase 1Flt-4fms-like tyrosine kinase 4RET receptorRet proto-oncogene

Inhibition of receptor tyrosine kinase activity, preventing ligand-induced phosphorylation and downstream signaling (anti-angiogenic/anti-lymphangiogenic effect) for VEGFR1/VEGFR3; Inhibition of RET tyrosine kinase, blocking pathological signaling, most often in cancer for RET.