Multi-kinase target profile (VEGFR1, VEGFR2, VEGFR3, TIE2, KIT, RET, PDGFR, FGFR, RAF, BRAF) (MKI Target Profile)

This target profile represents a comprehensive collection of kinases that are central to tumor progression, including members of the Vascular Endothelial Growth Factor Receptor family (VEGFR1/FLT1, VEGFR2/KDR, VEGFR3/FLT4) and TIE2 (TEK), which are essential for neoangiogenesis and lymphangiogenesis. It also includes key oncogenic drivers such as KIT (stem cell factor receptor), RET, and the RAF/BRAF serine/threonine kinases, which mediate the MAPK/ERK signaling pathway to promote cell proliferation and survival. Furthermore, the inclusion of Platelet-Derived Growth Factor Receptors (PDGFR) and Fibroblast Growth Factor Receptors (FGFR) highlights the role of these targets in modulating the tumor microenvironment and stromal cell signaling. Drugs that target this broad array of kinases, known as multi-kinase inhibitors (MKIs), are utilized to treat various advanced solid tumors by simultaneously disrupting multiple pathways that tumors use for growth and escape from therapy. This multi-targeted approach is particularly effective in heterogeneous malignancies like metastatic colorectal cancer, hepatocellular carcinoma, and renal cell carcinoma, where single-pathway inhibition is often insufficient. (Sources: UniProt P17948, P35968, P35916, Q02763, P10721, P07949, P16234, P15056; FDA Stivarga/Nexavar Prescribing Information; PubMed PMID: 23312468, 21170269).

Other names

Angiogenesis and proliferation kinase clusterReceptor tyrosine kinase (RTK) and serine/threonine kinase groupRegorafenib/Sorafenib target profileMulti-kinase inhibitor targets

Small molecule inhibition of the adenosine triphosphate (ATP) binding site across multiple receptor tyrosine kinases and intracellular serine/threonine kinases, effectively blocking downstream signaling pathways (such as MAPK/ERK and PI3K/AKT) that drive tumor angiogenesis, oncogenic growth, and stromal maintenance.