Kinetics and thermodynamics of dimer formation and dissociation for a recombinant humanized monoclonal antibody to vascular endothelial growth factor

Biochemistry. 1999 Oct 19;38(42):13960-7. doi: 10.1021/bi9905516.

Abstract

The recombinant humanized antibody (rhuMAb) VEGF has a high affinity for vascular endothelial growth factor and is currently being evaluated in clinical trials as a cancer therapeutic. Under acidic pH and low ionic strength conditions, the antibody was predominantly present as monomer. Under physiological conditions, the appearance of significant amounts of a noncovalent, reversible dimer were observed by size-exclusion chromatography. The kinetics and thermodynamics of the reversible self-association for rhuMAb VEGF monomer were investigated as a function of pH, temperature, and ionic strength by size-exclusion chromatography using the concentration jump method. The rate constant for dimer formation ranged 23-112 M(-)(1) min(-)(1) under the conditions studied, values that are significantly lower than those reported in the literature for other proteins that self-associate. The rate constant for dissociation ranged 0.0039-0.021 min(-)(1). Gibbs' free energies, enthalpies, entropies, and activation energies were determined and revealed that dimer formation is optimal at pH 7.5-8.0, which may be reflective of charge shielding occurring near the pI of the protein. There was a negative change in entropy for dissociation (values from -18.1 to -12.8 cal/mol K). In the presence of D(2)O or 1 M NaCl, dimerization was enhanced. The results of the kinetic and thermodynamic analysis of this study indicate that rhuMAb VEGF dimerization occurs primarily through hydrophobic interactions.

MeSH terms

  • Animals
  • Antibodies, Monoclonal / chemistry*
  • Antibodies, Monoclonal / genetics
  • Antibodies, Monoclonal / metabolism*
  • CHO Cells
  • Calcium Chloride / chemistry
  • Chromatography, Gel
  • Cricetinae
  • Dimerization
  • Endothelial Growth Factors / immunology*
  • Humans
  • Hydrogen-Ion Concentration
  • Kinetics
  • Light
  • Lymphokines / immunology*
  • Models, Chemical
  • Osmolar Concentration
  • Recombinant Proteins / chemistry*
  • Recombinant Proteins / metabolism*
  • Scattering, Radiation
  • Sodium Chloride / chemistry
  • Temperature
  • Thermodynamics
  • Vascular Endothelial Growth Factor A
  • Vascular Endothelial Growth Factors

Substances

  • Antibodies, Monoclonal
  • Endothelial Growth Factors
  • Lymphokines
  • Recombinant Proteins
  • Vascular Endothelial Growth Factor A
  • Vascular Endothelial Growth Factors
  • Sodium Chloride
  • Calcium Chloride