Fibroblast growth factor receptor 2 and Fibroblast growth factor receptor 3 (FGFR2 and FGFR3)

Fibroblast growth factor receptor 2 (FGFR2) and fibroblast growth factor receptor 3 (FGFR3) are members of the FGFR family of cell surface receptor tyrosine kinases. Each receptor spans the cell membrane and consists of an extracellular domain with three immunoglobulin-like subunits (for ligand binding), a single transmembrane helix, and an intracellular tyrosine kinase domain that transduces signals upon ligand binding and dimerization[1][2][3][4][5]. Both FGFR2 and FGFR3 regulate key biological processes such as cell proliferation, differentiation, development, tissue repair, and angiogenesis[1][2][3][4]. Genetic aberrations affecting these receptors (mutations, amplifications, fusions) are implicated in a variety of cancers (notably bladder, multiple myeloma, and others) and developmental diseases (such as skeletal dysplasias and craniosynostosis syndromes)[2][3]. These receptors are considered important therapeutic targets, and several FGFR inhibitors are approved or under investigation for cancer treatment, though challenges such as drug resistance and toxicity remain significant[3].

Other names

FGFR-2CD332FGFR-3CD333CEK2JTK4HBGFRFGR3_HUMAN

Small molecule inhibition of receptor tyrosine kinase activity (FGFR inhibitors block ATP binding, preventing signaling); Receptor dimerization antagonism (by some agents): preventing ligand-induced dimerization required for activation; Downregulation of aberrant FGFR-driven cell proliferation in tumors