Determination of binding constant of transcription factor AP-1 and DNA. Application of inhibitors

Eur J Biochem. 2001 Feb;268(3):565-72. doi: 10.1046/j.1432-1327.2001.01897.x.

Abstract

The equilibrium binding and association kinetics of the fos-jun dimer (basic and leucine zipper domain) to the AP-1 DNA were studied using a quantitative assay. The basic-region and leucine zipper (bZip) domain of c-fos was expressed as a fusion protein with glutathione S-transferase, and it was bound to glutathione-agarose. The GST-fused fos bZip region was allowed to form a heterodimer with the bZip domain of c-jun, to which radiolabeled AP-1 nucleotides were added. After thorough washing, the gel-bound radioactivity was counted. The binding and dissociation rate constants (k(1) and k-(1)) of the fos-jun dimer and DNA could be obtained from a time-course experiment. The association binding constant (K(1)) was determined using both a thermodynamic equation and kinetic parameters. Nordihydroguaiaretic acid (NDGA), momordin I, natural product inhibitors of the fos-jun/DNA complex formation, was applied to this jun-GST-fused fos system and it was found to decrease the apparent equilibrium binding of dimer and DNA. The thermodynamic constant of dimer and inhibitor binding was also determined.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cloning, Molecular
  • Cyclooxygenase Inhibitors / pharmacology
  • DNA / metabolism*
  • Dose-Response Relationship, Drug
  • Electrophoresis, Polyacrylamide Gel
  • Escherichia coli / metabolism
  • Glutathione / chemistry
  • Glutathione / metabolism
  • Glutathione Transferase / metabolism
  • Inhibitory Concentration 50
  • Kinetics
  • Masoprocol / pharmacology
  • Models, Biological
  • Oleanolic Acid / analogs & derivatives
  • Plasmids / metabolism
  • Protein Binding
  • Proto-Oncogene Proteins c-fos / chemistry
  • Recombinant Fusion Proteins / metabolism
  • Saponins / pharmacology
  • Sepharose / chemistry
  • Sepharose / metabolism
  • Sodium Chloride / pharmacology
  • Thermodynamics
  • Time Factors
  • Transcription Factor AP-1 / antagonists & inhibitors
  • Transcription Factor AP-1 / chemistry*
  • Transcription Factor AP-1 / metabolism

Substances

  • Cyclooxygenase Inhibitors
  • Proto-Oncogene Proteins c-fos
  • Recombinant Fusion Proteins
  • Saponins
  • Transcription Factor AP-1
  • momordin I (Oleanolic Acid)
  • Sodium Chloride
  • Oleanolic Acid
  • Masoprocol
  • DNA
  • Sepharose
  • Glutathione Transferase
  • Glutathione