Crystal structure of fibroblast growth factor 9 reveals regions implicated in dimerization and autoinhibition

J Biol Chem. 2001 Feb 9;276(6):4322-9. doi: 10.1074/jbc.M006502200. Epub 2000 Nov 1.

Abstract

Fibroblast growth factors (FGFs) constitute a large family of heparin-binding growth factors with diverse biological activities. FGF9 was originally described as glia-activating factor and is expressed in the nervous system as a potent mitogen for glia cells. Unlike most FGFs, FGF9 forms dimers in solution with a K(d) of 680 nm. To elucidate the molecular mechanism of FGF9 dimerization, the crystal structure of FGF9 was determined at 2.2 A resolution. FGF9 adopts a beta-trefoil fold similar to other FGFs. However, unlike other FGFs, the N- and C-terminal regions outside the beta-trefoil core in FGF9 are ordered and involved in the formation of a 2-fold crystallographic dimer. A significant surface area (>2000 A(2)) is buried in the dimer interface that occludes a major receptor binding site of FGF9. Thus, we propose an autoinhibitory mechanism for FGF9 that is dependent on sequences outside of the beta-trefoil core. Moreover, a model is presented providing a molecular basis for the preferential affinity of FGF9 toward FGFR3.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Binding Sites
  • Crystallography, X-Ray
  • Dimerization
  • Fibroblast Growth Factor 9
  • Fibroblast Growth Factors / antagonists & inhibitors
  • Fibroblast Growth Factors / chemistry*
  • Fibroblast Growth Factors / metabolism
  • Models, Molecular
  • Molecular Sequence Data
  • Protein Conformation
  • Receptors, Fibroblast Growth Factor / metabolism
  • Sequence Homology, Amino Acid

Substances

  • Fibroblast Growth Factor 9
  • Receptors, Fibroblast Growth Factor
  • Fibroblast Growth Factors