Fibroblast growth factor receptor 1 and 2 (FGFR1, FGFR2)

Fibroblast growth factor receptors (FGFRs) are single-pass transmembrane receptor tyrosine kinases that mediate the actions of fibroblast growth factors (FGFs). They are characterized structurally by having three immunoglobulin-like extracellular domains, a single transmembrane helix, and an intracellular split tyrosine kinase domain. FGFRs play a crucial role in embryogenesis, tissue repair, cell proliferation, differentiation, apoptosis, and angiogenesis. Aberrant FGFR signaling—by mutation, overexpression, or fusion—can drive tumorigenesis and other disease states. FGFRs are validated therapeutic targets, and multiple drugs are approved or in clinical development to inhibit their activity. FGFRs are also important in normal skeletal development, vascular biology, and organogenesis. FGFRA/FGFRB are not canonical receptor names; care should be taken to use the standard names (e.g., FGFR1, FGFR2) for structured annotation and database searches.

Other names

Fibroblast growth factor receptor 1Fibroblast growth factor receptor 2FGFR1FGFR2

Inhibition of tyrosine kinase activity; Blockage of FGF-FGFR binding; Autophosphorylation blockade; Downregulation of downstream signaling cascades (MAPK, AKT, STAT)