Thermodynamic analysis of the activation mechanism of the GCSF receptor induced by ligand binding

Biochemistry. 2004 Mar 9;43(9):2458-64. doi: 10.1021/bi0356855.

Abstract

The granulocyte colony-stimulating factor receptor (GCSFR), containing the Ig-like domain (Ig) and cytokine receptor homologous region (CRH), was prepared as a preformed dimer (Ig-CRH-Fc)(2) after fusion to the mouse Fc region via an eight-residue linker (approximately 55 A). Monomer Ig-CRH was also prepared after the Fc region was removed from (Ig-CRH-Fc)(2). GCSF binding to Ig-CRH and (Ig-CRH-Fc)(2) was investigated using light scattering and isothermal titration calorimetry. The average molecular mass determined by light scattering showed that both Ig-CRH and (Ig-CRH-Fc)(2) formed a 2:2 dimer with GCSF. Moreover, isothermal titration calorimetry showed that the thermodynamic parameters upon binding of GCSF to Ig-CRH and (Ig-CRH-Fc)(2) were comparable, suggesting a similar binding stoichiometry and interface [including similar buried surface area (5700-6000 A(2))] despite the presence of the eight-residue linker. The buried surface area is much larger than that calculated from our previous report of the crystal structure of the GCSF-CRH complex [Aritomi, M., et al. (1999) Nature 401, 713-717], suggesting a substantial contribution of the Ig domain to GCSF binding. The data also indicate that the distance (55 A) between two CRH domains in the 2:2 complex is much shorter than in our previous model (approximately 90 A) predicted from the same crystal structure of the GCSF-CRH complex.

MeSH terms

  • Animals
  • Baculoviridae / genetics
  • Calorimetry
  • Chromatography, Gel
  • Granulocyte Colony-Stimulating Factor / chemistry*
  • Granulocyte Colony-Stimulating Factor / metabolism*
  • Humans
  • Immunoglobulin Fc Fragments / genetics
  • Ligands
  • Light
  • Mice
  • Protein Binding / genetics
  • Protein Structure, Tertiary / genetics
  • Receptors, Cytokine / genetics
  • Receptors, Granulocyte Colony-Stimulating Factor / chemistry*
  • Receptors, Granulocyte Colony-Stimulating Factor / genetics
  • Receptors, Granulocyte Colony-Stimulating Factor / metabolism*
  • Recombinant Fusion Proteins / genetics
  • Recombinant Proteins
  • Scattering, Radiation
  • Solutions
  • Spodoptera / genetics
  • Structural Homology, Protein
  • Thermodynamics

Substances

  • Immunoglobulin Fc Fragments
  • Ligands
  • Receptors, Cytokine
  • Receptors, Granulocyte Colony-Stimulating Factor
  • Recombinant Fusion Proteins
  • Recombinant Proteins
  • Solutions
  • Granulocyte Colony-Stimulating Factor