Targeting anti-apoptotic Bcl2 proteins with scyllatoxin-based BH3 domain mimetics

Org Biomol Chem. 2016 Jan 14;14(2):440-446. doi: 10.1039/c5ob02080h.


BH3 domain mimetics based on the small protein scyllatoxin (ScTx) were designed to target the anti-apoptotic protein Bcl2 in vitro. Intrinsically disordered ScTx variants were found to bind Bcl2 with nanomolar affinity, indicating that an induced fit binding mechanism is required for favorable BH3 : Bcl2 interaction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biomimetic Materials / chemical synthesis
  • Biomimetic Materials / chemistry*
  • Biomimetic Materials / pharmacology*
  • Drug Design*
  • Models, Molecular
  • Protein Binding
  • Protein Structure, Tertiary
  • Proto-Oncogene Proteins c-bcl-2 / antagonists & inhibitors*
  • Proto-Oncogene Proteins c-bcl-2 / chemistry
  • Proto-Oncogene Proteins c-bcl-2 / metabolism*
  • Scorpion Venoms / chemistry*
  • Scorpion Venoms / metabolism


  • Proto-Oncogene Proteins c-bcl-2
  • Scorpion Venoms
  • leiurotoxin I