Fibroblast growth factor receptors 1, 2, 3, and 4 (FGFR1, FGFR2, FGFR3, FGFR4)

Fibroblast growth factor receptor 1, 2, 3, and 4 (FGFR1, FGFR2, FGFR3, FGFR4) are single-pass transmembrane receptor tyrosine kinases in the FGFR family, which bind to fibroblast growth factors (FGFs) and regulate signal transduction via activation of the kinase domain upon dimerization. Structurally, each receptor has an extracellular domain composed of three immunoglobulin-like domains (D1-D3), a transmembrane region, and an intracellular split tyrosine kinase domain. They are critical for embryonic development, cell proliferation, angiogenesis, and tissue repair; their dysregulation through mutation, amplification, or gene fusion contributes to cancer and various developmental diseases. Multiple drugs targeting these receptors are approved or in clinical development for cancers with FGFR alterations[1][2][3][4][5][6]. If you need information on one specific FGFR, please specify which subtype (FGFR1, FGFR2, FGFR3, or FGFR4).

Other names

FGFR-1FGFR-2FGFR-3FGFR-4CD331 (FGFR1)CD332 (FGFR2)CD333 (FGFR3)CD334 (FGFR4)FGF receptors

Reversible or irreversible inhibition of the intracellular tyrosine kinase domain, blocking receptor autophosphorylation and downstream signaling pathways (such as MAPK, PI3K-AKT, PLCγ, JAK/STAT)