One-pot hydrazide-based native chemical ligation for efficient chemical synthesis and structure determination of toxin Mambalgin-1

Chem Commun (Camb). 2014 Jun 4;50(44):5837-9. doi: 10.1039/c4cc00779d.

Abstract

An efficient one-pot chemical synthesis of snake venom toxin Mambalgin-1 was achieved using an azide-switch strategy combined with hydrazide-based native chemical ligation. Synthetic Mambalgin-1 exhibited a well-defined structure after sequential folding in vitro. NMR spectroscopy revealed a three-finger toxin family structure, and the synthetic toxin inhibited human acid-sensing ion channel 1a.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acid Sensing Ion Channels / drug effects
  • Azides / chemistry*
  • Elapid Venoms / chemical synthesis*
  • Elapid Venoms / chemistry
  • Elapid Venoms / toxicity
  • Models, Molecular
  • Nuclear Magnetic Resonance, Biomolecular
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Peptides / toxicity
  • Protein Conformation

Substances

  • ASIC1 protein, human
  • Acid Sensing Ion Channels
  • Azides
  • Elapid Venoms
  • Peptides
  • mambalgin-1, Dendroaspis polylepis