Figure 2. Inhibition of receptor kinases via ligand-binding site inhibition.

Receptor kinases can be activated by extracellular signals that bind the ectodomain of the kinase. These extracellular ligand-binding sites can be selectively targeted to ultimately inhibit kinase activation. Examples include the interaction between PDGF and PDGFR, EGF and EGFR, HGF and the Met receptor and VEGF and VEGFR.