Utilization of a nitrobenzoxadiazole (NBD) fluorophore in the design of a Grb2 SH2 domain-binding peptide mimetic

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1385-8. doi: 10.1016/j.bmcl.2005.01.017.


Fluorescence labeling has become a general technique for studying the intracellular accumulation and localization of exogenously administered materials. Reported herein is a low nanomolar affinity Grb2 SH2 domain-binding antagonist that utilizes the environmentally-sensitive nitrobenzoxadiazole (NBD) fluorophore as a naphthyl replacement. This novel agent should serve as a useful tool to visualize the actions of this class of Grb2 SH2 domain-binding antagonists in whole cell systems.

MeSH terms

  • Adaptor Proteins, Signal Transducing / antagonists & inhibitors*
  • Binding, Competitive
  • Drug Design
  • Fluorescent Dyes / chemical synthesis
  • Fluorescent Dyes / chemistry*
  • GRB2 Adaptor Protein
  • Ligands
  • Molecular Conformation
  • Molecular Mimicry
  • Oxadiazoles / chemical synthesis
  • Oxadiazoles / chemistry*
  • Peptides / chemistry*
  • Peptides / pharmacology*
  • Protein Binding / drug effects
  • Staining and Labeling / methods
  • Structure-Activity Relationship
  • src Homology Domains / drug effects*


  • Adaptor Proteins, Signal Transducing
  • Fluorescent Dyes
  • GRB2 Adaptor Protein
  • Ligands
  • Oxadiazoles
  • Peptides