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

Fibroblast growth factor receptors 1 through 3 (FGFR1, FGFR2, FGFR3) are members of the receptor tyrosine kinase family that serve as high-affinity cell-surface receptors for fibroblast growth factors. They play essential roles in regulating cell proliferation, differentiation, embryonic development, angiogenesis, tissue homeostasis, metabolism, wound healing, and bone formation. Each receptor spans the plasma membrane with an extracellular ligand-binding domain and an intracellular split tyrosine kinase domain that initiates signal transduction upon activation by its ligands. Alternative splicing generates multiple isoforms with distinct tissue distributions and ligand affinities. Genetic alterations—such as activating mutations or gene fusions—in these receptors can lead to constitutive activation independent of ligand binding. This aberrant signaling is implicated in various diseases including skeletal dysplasias and several cancers such as bladder cancer, multiple myeloma, cervical cancer, clonal eosinophilias, among others. As a result of their central role in oncogenic signaling pathways like PI3K/AKT/mTOR and MAPK/ERK cascades,[3] they have become important therapeutic targets; several small-molecule inhibitors targeting these kinases have been developed or approved for clinical use.[1][2][4]

Other names

CD331 (FGFR1)CD332 (FGFR2)CD333 (FGFR3)Basic fibroblast growth factor receptor 1Fms-related tyrosine kinase-2Pfeiffer syndrome gene (FGFR1)ACH (FGFR3)CEK2 (FGFR3)HBGFR (FGFR3)JTK4 (FGFR3)

Inhibition of the tyrosine kinase activity of FGFRs to block downstream signaling pathways involved in cell proliferation and survival