Sometimes, a dysregulation of Fibroblast Growth Factors (FGFs) may occur and causes cancer. The dysregulations usually fall into six categories: (1) a specific FGF ligand is overproduced; (2) the specificity of splice-variant FGFRs to endogenous FGF ligands have changed; (3) FGFRs are mutated, resulting in receptor dimerization or constitutive activation of the kinase; (4) there is a gene translocation in FGFRs that leads to over-expression or activation of the FGFR; (5) germline SNPs exist, which are related with increased risk of cancer; (6) the impairment of the normal attenuation and negative feedback. Considering this, it is no doubt that researchers are pursuing to generate agents to control FGF-ligand/receptor dysregulation.
Table 2. Current clinical development status of FGF/FGFR-targeting anticancer agents