Fibroblast growth factor 1 receptor (FGFR1)

Fibroblast growth factor receptor 1 (FGFR1) is a cell-surface tyrosine kinase receptor that binds members of the fibroblast growth factor (FGF) family, particularly fibroblast growth factor 1 (FGF-1, also called acidic FGF), mediating diverse biological processes including embryonic development, cell proliferation, differentiation, survival, and angiogenesis[2][3][5][6][7]. FGFR1 contains extracellular immunoglobulin-like domains for ligand binding, a single transmembrane domain, and an intracellular tyrosine kinase domain, which activates downstream signaling cascades such as the MAPK, PI3K/AKT, and PLCγ pathways upon ligand-induced dimerization[3][5][6]. FGFR1 is a well-established therapeutic target in oncology, especially in tumors harboring FGFR1 gene amplification or activating mutations, and is also implicated in developmental and metabolic diseases[2][5][6]. Multiple small-molecule inhibitors targeting FGFR1 have been developed and approved for cancer therapy, but the clinical use is associated with specific on-target toxicities that require careful patient management.

Other names

Fibroblast growth factor receptor 1CD331bFGF receptor 1FLGFGF receptor 1FGF-1 receptor

Small-molecule inhibitors (block the kinase activity of FGFR1 and downstream signaling) Monoclonal antibodies (block ligand binding or receptor dimerization) Ligand traps (sequester ligand away from the receptor)