Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 2, Fibroblast growth factor receptor 3 (FGFR1, FGFR2, FGFR3)

FGFR1, FGFR2, and FGFR3 are members of the fibroblast growth factor receptor family, part of the receptor tyrosine kinase superfamily. Each receptor has an extracellular domain with three immunoglobulin-like domains responsible for binding fibroblast growth factors, a single transmembrane helix, and an intracellular tyrosine kinase domain responsible for signal transduction after ligand-induced dimerization and autophosphorylation. They play essential roles in tissue development, angiogenesis, cellular proliferation, and differentiation. Dysregulation (mutation or overexpression) of these receptors is implicated in cancer (via promoting proliferation and survival), developmental disorders, and other diseases. Multiple drugs target these receptors, primarily in oncology, by inhibiting their kinase activity.

Other names

CD331CD332CD333FGFR-1FGFR-2FGFR-3FGF receptor 1FGF receptor 2FGF receptor 3

Competitive inhibition of the ATP-binding site in the tyrosine kinase domain (TKI mechanism) Inhibition of FGFR phosphorylation and downstream signaling (prevents MAPK/ERK, PI3K/AKT pathways)