VEGFR-2, FGFR, PDGFR, c-Kit

These targets are all receptor tyrosine kinases that play critical roles in mediating cell signaling pathways involved in angiogenesis, cellular proliferation, survival, and migration. Dysregulation or overexpression of these receptors is implicated in various cancers and other proliferative diseases. Therapeutic inhibition of VEGFR-2, PDGFR (α/β), FGFRs, or c-Kit can suppress tumor growth and angiogenesis, but presents safety concerns due to their functions in normal physiology. Small molecule inhibitors and monoclonal antibodies against these receptors form a major part of anti-angiogenic and targeted cancer therapies[1][2][4][5][6].

Other names

KDRFlk-1FGFR1FGFR2FGFR3FGFR4PDGFRαPDGFRβKITCD117Stem cell factor receptor

These mechanisms primarily involve kinase inhibition, blocking ATP-binding to the tyrosine kinase domain, which prevents phosphorylation and subsequent downstream signaling. This leads to downregulation of angiogenesis, suppression of cell proliferation and survival signals, and interference with tumor vasculature.