Reduced binding of FGF1 to mutant fibroblast growth factor receptor 3

Growth Factors. 2006 Jun;24(2):111-9. doi: 10.1080/08977190600621388.

Abstract

The activating mutation FGFR3-R248C in the D2-D3 linker region of fibroblast growth factor receptor 3 leads as germline mutation to the neonatal lethal syndrome thanatophoric dysplasia type I (TD1). As somatic mutation it has been found in cancer. We introduced into the murine FGFR3 the mutation R242C that is orthologoues to the human mutation R248C. A strong reduction in binding of the 16 and 18 kDa forms of FGF1 to the mutant receptor was found, highlighting the importance of D2-D3 linker region of FGFR3 in determination of binding affinity to ligands. Another mutant, G374R, introduced into the murine FGFR3, is orthologoues to the human mutant FGFR3-G380R, and leads to achondroplasia (ACH). The binding of the 16 kDa and 18 kDa forms of FGF1 to this mutant receptor was the same as for wild-type FGFR3 in a cell-free system, but it was reduced in living cells. The data indicate a minor changes in conformation of FGFR3-G374R receptors at the cell surface that lead to reduced binding to FGF1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Achondroplasia / genetics
  • Achondroplasia / metabolism
  • Animals
  • Cells, Cultured
  • Fibroblast Growth Factor 1 / metabolism*
  • Gene Expression
  • Mice
  • Mutation
  • Receptor, Fibroblast Growth Factor, Type 3 / genetics
  • Receptor, Fibroblast Growth Factor, Type 3 / metabolism*
  • Thanatophoric Dysplasia / genetics
  • Thanatophoric Dysplasia / metabolism

Substances

  • Fibroblast Growth Factor 1
  • Receptor, Fibroblast Growth Factor, Type 3