Evans Blue Is an Inhibitor of Nuclear Factor-Kappa B (NF-kappaB)-DNA Binding

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6123-7. doi: 10.1016/j.bmcl.2004.07.096.

Abstract

Nuclear factor-kappa B (NF-kappaB) is an important transcription factor, involved in many immune and inflammatory responses. It is critical in HIV gene expression as it has kappa B binding sites in the HIV-1 long-terminal repeat. Hence, targeting NF-kappaB to prevent its DNA binding holds a significant therapeutic potential. In this context, we report Evans Blue as a novel inhibitor of NF-kappaB-DNA binding. Evans Blue was found to be inhibiting DNA binding of NF-kappaB at a low concentration of 100 microM. Further, molecular modeling studies using docking and generation of electrostatic potential maps predicted a possible binding mode of EB to the DNA binding region of NF-kappaB, consistent with the experimental activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Nucleus / chemistry*
  • DNA / antagonists & inhibitors*
  • DNA / chemistry
  • DNA / metabolism
  • Dose-Response Relationship, Drug
  • Electrophoretic Mobility Shift Assay / methods
  • Evans Blue / chemistry
  • Evans Blue / pharmacology*
  • Models, Molecular
  • Molecular Structure
  • NF-kappa B / antagonists & inhibitors*
  • NF-kappa B / metabolism
  • Protein Binding / drug effects
  • Structure-Activity Relationship

Substances

  • NF-kappa B
  • Evans Blue
  • DNA