FGFR Signaling and Targeting FGFR

    • Fibroblast growth factor receptors (FGFRs) family has four highly conserved transmembrane RTKs (FGFR1–4) that differ in their ligand affinities and tissue distribution.
    • Fibroblast growth factors (FGFs) include 18 structurally related polypeptides (FGF1–10, FGF16–23) that signal through FGFRs.
    • FGFRs can bind canonical FGFs that are in complex with heparan sulfate proteoglycans (HSPGs) in an autocrine and paracrine fashion.
    • FGFRs can also bind endocrine FGFs (FGF19, 21, and 23) that are found in circulation, free of HSPGs.
    • Once bound to their ligands, FGFRs are induced to dimerize and cross-phosphorylate the tyrosine kinase domain the cognate receptor.
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