ABSTRACT

Introduction ............................................................................................................ 158 FGF/FGFR Signaling ............................................................................................. 158 FGF/FGFR Pathway Functions .............................................................................. 158 Mechanisms for FGF/FGFR Signaling Dysregulation in Human Cancer ............. 159

Hematologic Diseases ....................................................................................... 160 Breast Cancer .................................................................................................... 160 Genitourinary Cancers ...................................................................................... 161 Gynecological Cancers...................................................................................... 161 Lung Cancer ...................................................................................................... 161 Gastrointestinal Cancers.................................................................................... 162 Hepatocellular Carcinoma ................................................................................. 162 Other Cancers .................................................................................................... 162

Targeting FGF Pathway in the Clinic ..................................................................... 163 Small-Molecule Tyrosine Kinase Inhibitors ..................................................... 164

Nonselective FGFR TKIs ............................................................................. 164 Selective Anti-FGFR TKIs ........................................................................... 166

Monoclonal Antibodies and FGF-Ligand Traps ............................................... 167 Conclusions ............................................................................................................ 167 References .............................................................................................................. 168

The signaling pathway mediated by the fibroblast growth factor receptors (FGFRs) and their ligands fibroblast growth factors (FGFs) regulates key functions in human physiology. Alterations of FGF signaling have been linked to different human diseases including cancer. These observations suggested that this pathway may represent a potential target for anticancer therapies.