Various Kinase Therapeutic Targets

The listed molecules are key regulators of cell signaling, primarily through their function as receptor tyrosine kinases or cytoplasmic protein kinases. They control processes central to embryogenesis, angiogenesis, tissue growth and repair, and oncogenic transformation. Aberrant activity or mutation of these kinases drives oncogenesis and is associated with poor prognosis in numerous solid and hematologic cancers. Targeted therapies (typically small-molecule kinase inhibitors) have revolutionized the treatment landscape for diseases involving these pathways, but face challenges including drug resistance, side effects, and limited efficacy for certain tumor types[1][2][4][5][6].

Other names

B-RAFRAF1 (C-RAF)A-RAFFLT1 (VEGFR1)KDR/FLK1 (VEGFR2)FLT4 (VEGFR3)CD140bCD135CD117Stem cell factor receptorSCFRc-KITRET proto-oncogeneFGF receptor 1

Inhibition of tyrosine kinase activity—these drugs bind ATP sites or allosteric sites of kinases, preventing downstream phosphorylation and activation of signal transduction pathways, thus blocking cellular proliferation, angiogenesis, or other cancer-promoting processes. Type I (ATP-competitive), Type II (inactive-kinase), Type III (allosteric), and experimental Type IV/V inhibitors.